I. Gilbert

发表

Automated design of ligands to polypharmacological profiles

Maria F. Sassano, G. R. Bickerton, Jérémy Besnard, 2012, Nature.

Virtual fragment screening for novel inhibitors of 6-phosphogluconate dehydrogenase

G. F. Ruda, I. Gilbert, Gordon Campbell, 2010, Bioorganic & medicinal chemistry.

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

Ian H. Gilbert, David Horn, Mark C. Field, 2017, Nature Reviews Microbiology.

Lessons Learnt from Assembling Screening Libraries for Drug Discovery for Neglected Diseases

Daniel James, Agata Krasowski, Ruth Brenk, 2007, ChemMedChem.

Small Polar Hits against S. aureus: Screening, Initial Hit Optimization, and Metabolomic Studies

Isabel M. Vincent, I. Gilbert, M. Barrett, 2019, ACS omega.

Synthesis and biological evaluation of substrate-based inhibitors of 6-phosphogluconate dehydrogenase as potential drugs against African trypanosomiasis.

Stefania Hanau, Christophe Dardonville, Michael P Barrett, 2003, Bioorganic & medicinal chemistry.

Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3

Ian H Gilbert, Paul G Wyatt, Torsten Luksch, 2011, ChemMedChem.

Kinetic Characterization of Squalene Synthase from Trypanosoma cruzi: Selective Inhibition by Quinuclidine Derivatives

I. Gilbert, J. Urbina, R. Brun, 2007, Antimicrobial Agents and Chemotherapy.

Potential application of thymidylate kinase in nucleoside analogue activation in Plasmodium falciparum.

I. Gilbert, D. González-Pacanowska, H. Cui, 2010, Bioorganic & medicinal chemistry.

Inhibitors of dihydrofolate reductase in Leishmania and trypanosomes.

I. Gilbert, 2002, Biochimica et biophysica acta.

Novel inhibitors of Trypanosoma cruzi dihydrofolate reductase.

M. Zvelebil, I. Gilbert, L. Maes, 2001, European journal of medicinal chemistry.

Assay donovani Assay with an Axenic Amastigote High-Content Intracellular Leishmania Comparison of a High-Throughput

Lorna, S. Cameron, I. Gilbert, 2013 .

AssayAssay with an Axenic Amastigote High-Content Intracellular Leishmania Comparison of a High-Throughput

S. Cameron, I. Gilbert, D. Gray, 2013 .

Synthesis and Evaluation of 1-(1-(Benzo[b]thiophen-2-yl)cyclohexyl)piperidine (BTCP) Analogues as Inhibitors of Trypanothione Reductase

I. Gilbert, A. Fairlamb, P. Wyatt, 2009, ChemMedChem.

Challenges and recent progress in drug discovery for tropical diseases

I. Gilbert, M. D. Rycker, S. Duce, 2018, Nature.

Challenges and recent progress in drug discovery for tropical diseases

I. Gilbert, S. Duce, M. De Rycker, 2018, Nature.

A novel multiple-stage antimalarial agent that inhibits protein synthesis

David W. Gray, E. Winzeler, S. Meister, 2015, Nature.

Design, synthesis and evaluation of potential inhibitors of HIV gp120-CD4 interactions.

I. Gilbert, T. Klimkait, N. Mahmood, 2004, Bioorganic & medicinal chemistry letters.

Solid-phase synthesis of diamine and polyamine amino acid derivatives as HIV-1 tat-TAR binding inhibitors.

I. Gilbert, T. Klimkait, C. Simons, 2003, Bioorganic & medicinal chemistry.

Pharmacological Validation of N-Myristoyltransferase as a Drug Target in Leishmania donovani

L. Stojanovski, K. Read, I. Gilbert, 2018, ACS infectious diseases.

Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis

Michael D. Urbaniak, David W. Gray, G. Drewes, 2018, Nature.

High Throughput Phenotypic Screening of The Human Spermatozoon.

J. Swedlow, I. Gilbert, Neil R. Norcross, 2021, Reproduction.

2,4-Diaminopyrimidines as inhibitors of Leishmanial and Trypanosomal dihydrofolate reductase.

I. Gilbert, V. Yardley, S. Croft, 2003, Bioorganic & medicinal chemistry.

Characterising covalent warhead reactivity

I. Gilbert, James S. Martin, C. Mackenzie, 2019, Bioorganic & medicinal chemistry.

Clinical and veterinary trypanocidal benzoxaboroles target CPSF3

Mark C. Field, I. Gilbert, D. Horn, 2018, Proceedings of the National Academy of Sciences.

Identification of a Proteasome-Targeting Arylsulfonamide with Potential for the Treatment of Chagas’ Disease

I. Gilbert, D. Horn, L. S. Torrie, 2021, Antimicrobial agents and chemotherapy.

Targeted delivery of compounds to Trypanosoma brucei using the melamine motif.

I. Gilbert, M. Barrett, P. E. Wong, 2009, Bioorganic & medicinal chemistry.

Imidazolines as amide bond replacements

I. Gilbert, Raymond C. F. Jones, D. Rees, 1995 .

Optimisation of a key cross-coupling reaction towards the synthesis of a promising antileishmanial compound

I. Gilbert, A. Moure, Michael G. Thomas, 2019, Tetrahedron letters.

Squalamine analogues as potential anti-trypanosomal and anti-leishmanial compounds.

I. Gilbert, V. Yardley, S. Croft, 2000, Bioorganic & medicinal chemistry letters.

Design, synthesis and evaluation of 2,4-diaminoquinazolines as inhibitors of trypanosomal and leishmanial dihydrofolate reductase.

I. Gilbert, R. Brun, D. González-Pacanowska, 2005, Bioorganic & medicinal chemistry.

Investigation of acyclic uridine amide and 5′-amido nucleoside analogues as potential inhibitors of the Plasmodium falciparum dUTPase☆

I. Gilbert, A. Schipani, D. González-Pacanowska, 2013, Bioorganic & medicinal chemistry.

Kinetic properties and inhibition of the dimeric dUTPase-dUDPase from Campylobacter jejuni

I. Gilbert, K. Wilson, A. E. Vidal, 2009, Journal of enzyme inhibition and medicinal chemistry.

Mechanistic Insights into the Cure of Prion Disease by Novel Antiprion Compounds

I. Gilbert, T. Wisniewski, David R. Brown, 2007, Journal of Virology.

Investigation of copper(II) tetrafluoroborate catalysed epoxide opening

I. Gilbert, M. Ferguson, Arthur T. Crossman, 2011, Tetrahedron letters.

Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs

Robert H Bates, L. Stojanovski, K. Read, 2022, Nature Communications.

Toolkit of Approaches To Support Target-Focused Drug Discovery for Plasmodium falciparum Lysyl tRNA Synthetase

I. Gilbert, D. Robinson, L. S. Torrie, 2022, ACS infectious diseases.

Male contraceptive development: A medicinal chemistry perspective.

J. Swedlow, K. Read, I. Gilbert, 2022, European journal of medicinal chemistry.

Anti-trypanosomatid drug discovery: progress and challenges

K. Read, I. Gilbert, D. Horn, 2022, Nature reviews. Microbiology.

Discovery and Optimization of a Compound Series Active against Trypanosoma cruzi, the Causative Agent of Chagas Disease.

Ana Rodriguez, L. Stojanovski, K. Read, 2020, Journal of medicinal chemistry.

Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity: Initial SAR and Assessment of In Vivo Activity

S. Norval, Frederick R. C. Simeons, L. Stojanovski, 2020, Journal of medicinal chemistry.

University of Dundee Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity

S. Norval, Frederick R. C. Simeons, L. Stojanovski, 2020 .

Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma

A. Hill, Frederick R. C. Simeons, L. Stojanovski, 2017 .

Lewis acid-catalysed rearrangements of myo-inositol orthoformate derivatives

I. Gilbert, A. Holmes, M. Pestchanker, 1992 .

General synthesis of 3-phosphorylated myo-inositol phospholipids and derivatives

I. Gilbert, P. Hawkins, L. Stephens, 1999 .

VERSATILE SYNTHESIS OF MYO-INOSITOL PHOSPHOLIPID PRECURSORS

I. Gilbert, A. Holmes, G. Painter, 1997 .

Synthesis of protected myo-inositols

I. Gilbert, A. Holmes, R. C. Young, 1990 .

Exhaustive sampling of the fragment space associated to a molecule leading to the generation of conserved fragments

I. Gilbert, Kathrin Heikamp, F. Zuccotto, 2017, Chemical biology & drug design.

Azasterols impair Giardia lamblia proliferation and induces encystation.

I. Gilbert, W. de Souza, M. Attias, 2007, Biochemical and biophysical research communications.

Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif

Farah El Mazouni, I. Gilbert, M. Barrett, 2010, Bioorganic & medicinal chemistry letters.

Water-soluble polymer–drug conjugates for combination chemotherapy against visceral leishmaniasis

I. Gilbert, K. Seifert, S. Nicoletti, 2010, Bioorganic & medicinal chemistry.

N-(2-hydroxypropyl)methacrylamide–amphotericin B (HPMA–AmB) copolymer conjugates as antileishmanial agents

I. Gilbert, K. Seifert, S. Nicoletti, 2009, International journal of antimicrobial agents.

Identification and development of a series of disubstituted piperazines for the treatment of Chagas disease.

Peter G. Dodd, Frederick R. C. Simeons, L. Stojanovski, 2022, European journal of medicinal chemistry.

High-Throughput Screening Platform To Identify Inhibitors of Protein Synthesis with Potential for the Treatment of Malaria

Fernando Sánchez-Román Terán, I. Gilbert, J. Baum, 2022, Antimicrobial agents and chemotherapy.

Design, synthesis and evaluation of peptide libraries as potential anti-HIV compounds, via inhibition of gp120/cell membrane interactions, using the gp120/cd4/fab17 crystal structure.

I. Gilbert, T. Klimkait, N. Mahmood, 2002, European journal of medicinal chemistry.

Synthesis of β-keto and α,β-unsaturated N-acetylcysteamine thioesters

I. Gilbert, J. Staunton, T. J. Simpson, 1995 .

Deoxyuridine triphosphate nucleotidohydrolase as a potential antiparasitic drug target.

I. Gilbert, R. Brun, D. González-Pacanowska, 2005, Journal of medicinal chemistry.

Squalamine Analogues as Potential Anti‐Trypanosomal and Anti‐Leishmanial Compounds.

I. Gilbert, V. Yardley, S. Croft, 2000 .

Modified 5′‐Trityl Nucleosides as Inhibitors of Plasmodium falciparum dUTPase

G. F. Ruda, I. Gilbert, R. Brun, 2011, ChemMedChem.

Synthetic arylquinuclidine derivatives exhibit antifungal activity against Candida albicans, Candida tropicalis and Candida parapsilopsis

I. Gilbert, W. de Souza, J. Urbina, 2011, Annals of Clinical Microbiology and Antimicrobials.

Electrospray Mass Spectrometry for Assay of Erythromycin A Extracted From Fermentation Liquor

I. Gilbert, D. Lloyd, R. Rowlands, 1998 .

University of Dundee Chemical Validation of Methionyl tRNA Synthetase ( MetRS ) as a Druggable Target in Leishmania donovani

Frederick R. C. Simeons, L. Stojanovski, K. Read, 2017 .

Targeting of toxic compounds to the trypanosome's interior.

I. Gilbert, M. Barrett, 2006, Advances in parasitology.

Dihydroquinazolines as a Novel Class of Trypanosoma brucei Trypanothione Reductase Inhibitors: Discovery, Synthesis, and Characterization of their Binding Mode by Protein Crystallography

Ian H. Gilbert, Alan H. Fairlamb, Paul G. Wyatt, 2011, Journal of medicinal chemistry.

Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.

I. Gilbert, M. Barrett, V. Yardley, 2005, Journal of medicinal chemistry.

Synthesis of analogues of Congo red and evaluation of their anti-prion activity.

I. Gilbert, David R. Brown, C. Birkett, 2004, Journal of medicinal chemistry.

Synthesis and evaluation of analogues of Congo red as potential compounds against transmissible spongiform encephalopathies.

James Hope, Ian H Gilbert, I. Gilbert, 2003, European journal of medicinal chemistry.

Towards the sustainable discovery and development of new antibiotics

H. Petković, I. Gilbert, M. Lindvall, 2021, Nature Reviews Chemistry.

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis

Juan A. Bueren-Calabuig, Andrei V. Pisliakov, David W. Gray, 2019, Proceedings of the National Academy of Sciences.

Biochemical and Structural Characterization of Selective Allosteric Inhibitors of the Plasmodium falciparum Drug Target, Prolyl-tRNA-synthetase

David W. Gray, K. Read, I. Gilbert, 2016, ACS infectious diseases.

Structure–Activity Relationship Studies of Pyrrolone Antimalarial Agents

Marcel Kaiser, Susan A Charman, Ian H Gilbert, 2013, ChemMedChem.

Discovery and Structure–Activity Relationships of Pyrrolone Antimalarials

Ian H. Gilbert, Marcel Kaiser, David M. Shackleford, 2013, Journal of medicinal chemistry.

Synthesis of (R)-2-methyl-4-deoxy and (R)-2-methyl-4,5-dideoxy analogues of 6-phosphogluconate as potential inhibitors of 6-phosphogluconate dehydrogenase.

I. Gilbert, C. Dardonville, 2003, Organic & biomolecular chemistry.

Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy

David W. Gray, E. Winzeler, S. Meister, 2016, Journal of medicinal chemistry.

Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials

E. Winzeler, S. Meister, S. Norval, 2016, Journal of medicinal chemistry.

Design, synthesis and evaluation of novel uracil acetamide derivatives as potential inhibitors of Plasmodium falciparum dUTP nucleotidohydrolase.

I. Gilbert, R. Brun, M. Kaiser, 2009, European journal of medicinal chemistry.

Design and preparation of sterol mimetics as potential antiparasitics.

Marcel Kaiser, Federica Gigante, Ian H Gilbert, 2010, Bioorganic & medicinal chemistry.

SAR studies on azasterols as potential anti-trypanosomal and anti-leishmanial agents.

I. Gilbert, R. Brun, M. Kaiser, 2009, Bioorganic & medicinal chemistry.

Evaluation of azasterols as anti-parasitics.

I. Gilbert, V. Yardley, S. Croft, 2006, Journal of medicinal chemistry.

New Azasterols against Trypanosoma brucei: Role of 24-Sterol Methyltransferase in Inhibitor Action

I. Gilbert, V. Yardley, S. Croft, 2006, Antimicrobial Agents and Chemotherapy.

Preparation of transition-state analogues of sterol 24-methyl transferase as potential anti-parasitics.

I. Gilbert, V. Yardley, S. Croft, 2005, Bioorganic & medicinal chemistry.

Novel Azasterols as Potential Agents for Treatment of Leishmaniasis and Trypanosomiasis

I. Gilbert, V. Yardley, S. Croft, 2004, Antimicrobial Agents and Chemotherapy.

Azasterols as inhibitors of sterol 24-methyltransferase in Leishmania species and Trypanosoma cruzi.

I. Gilbert, V. Yardley, S. Croft, 2003, Journal of medicinal chemistry.

From On-Target to Off-Target Activity: Identification and Optimisation of Trypanosoma brucei GSK3 Inhibitors and Their Characterisation as Anti-Trypanosoma brucei Drug Discovery Lead Molecules

I. Gilbert, R. Brenk, P. Wyatt, 2013, ChemMedChem.

One Scaffold, Three Binding Modes: Novel and Selective Pteridine Reductase 1 Inhibitors Derived from Fragment Hits Discovered by Virtual Screening

Ian H. Gilbert, Chidochangu P. Mpamhanga, William N. Hunter, 2009, Journal of medicinal chemistry.

Acetazolamide-based fungal chitinase inhibitors

Ian H. Gilbert, I. Gilbert, A. W. Schüttelkopf, 2010, Bioorganic & medicinal chemistry.

Characterization of a Melamino Nitroheterocycle as a Potential Lead for the Treatment of Human African Trypanosomiasis

I. Gilbert, M. Barrett, C. Pellacani, 2014, Antimicrobial Agents and Chemotherapy.

Quinol derivatives as potential trypanocidal agents

I. Gilbert, A. Fairlamb, P. Wyatt, 2012, Bioorganic & medicinal chemistry.

Novel functionalized melamine-based nitroheterocycles: synthesis and activity against trypanosomatid parasites.

I. Gilbert, M. Barrett, R. Brun, 2009, Organic & biomolecular chemistry.

Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.

I. Gilbert, M. Barrett, V. Yardley, 2005, Journal of medicinal chemistry.

Synthesis and biological evaluation of s-triazine substituted polyamines as potential new anti-trypanosomal drugs.

I. Gilbert, M. Barrett, R. Brun, 2001, Journal of medicinal chemistry.

dUTPase as a platform for antimalarial drug design: structural basis for the selectivity of a class of nucleoside inhibitors.

I. Gilbert, K. Wilson, A. Wilkinson, 2005, Structure.

Amide bond replacements : incorporation of a 2,5,5-trisubstituted imidazoline into dipeptides and into a CCK-4 derivative.

I. Gilbert, D. Rees, R. Richardson, 1991 .

Analogues of thiolactomycin as potential antimalarial agents.

I. Gilbert, J. Harwood, R. Brun, 2005, Journal of medicinal chemistry.

Synthesis of a Series of Diaminoindoles

I. Gilbert, Claire J. Mackenzie, James S Martin, 2021, The Journal of organic chemistry.

Synthesis of a homochiral α,α-disubstituted α,β-diamino-acid

I. Gilbert, D. Rees, Alan K. Crockett, 1994 .

Fragment screening reveals salicylic hydroxamic acid as an inhibitor of Trypanosoma brucei GPI GlcNAc-PI de-N-acetylase

Michael D. Urbaniak, I. Gilbert, M. Ferguson, 2014, Carbohydrate research.

Rapid and sensitive quantitation of antibiotics in fermentations by electrospray mass spectrometry.

D Lloyd, I. Gilbert, D. Lloyd, 2001, Rapid communications in mass spectrometry : RCM.

Perspectives for new drugs against trypanosomiasis and leishmaniasis.

I. Gilbert, M. Barrett, 2002, Current topics in medicinal chemistry.

The Qi Site of Cytochrome b is a Promiscuous Drug Target in Trypanosoma cruzi and Leishmania donovani

Juan A. Bueren-Calabuig, I. Gilbert, A. Fairlamb, 2020, ACS infectious diseases.

Comparison of a High-Throughput High-Content Intracellular Leishmania donovani Assay with an Axenic Amastigote Assay

S. Cameron, I. Gilbert, A. Fairlamb, 2013, Antimicrobial Agents and Chemotherapy.

Alterations on the growth and ultrastructure of Leishmania chagasi induced by squalene synthase inhibitors.

I. Gilbert, W. de Souza, J. Urbina, 2007, Veterinary parasitology.

Quinuclidine Derivatives as Potential Antiparasitics

I. Gilbert, J. Urbina, R. Brun, 2007, Antimicrobial Agents and Chemotherapy.

Effects of Inhibitors of Δ24(25)-Sterol Methyl Transferase on the Ultrastructure of Epimastigotes of Trypanosoma cruzi

I. Gilbert, W. de Souza, F. Magaraci, 2005, Microscopy and Microanalysis.

Biphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa.

I. Gilbert, V. Yardley, S. Croft, 2005, Bioorganic & medicinal chemistry.

Multiple unbiased approaches identify oxidosqualene cyclase as the molecular target of a promising anti-leishmanial

I. Gilbert, A. Fairlamb, M. Ferguson, 2021, Cell chemical biology.

Trypanocidal Activity of Melamine-Based Nitroheterocycles

I. Gilbert, M. Barrett, R. Brun, 2004, Antimicrobial Agents and Chemotherapy.

Plasmodium Kinases as Potential Drug Targets for Malaria: Challenges and Opportunities

I. Gilbert, K. Chibale, S. Wyllie, 2021, ACS infectious diseases.

The design and synthesis of nucleoside triphosphate isosteres as potential inhibitors of HIV reverse transcriptase

I. Gilbert, R. Weaver, 1997 .

Fragment-based hit identification: thinking in 3D.

Nathan Brown, Steven V Ley, Kristian Birchall, 2013, Drug discovery today.

Repositioning of a Diaminothiazole Series Confirmed to Target the Cyclin-Dependent Kinase CRK12 for Use in the Treatment of African Animal Trypanosomiasis

Frederick R. C. Simeons, L. Stojanovski, K. Read, 2022, Journal of medicinal chemistry.

Interaction of Monobenzamidine-Linked Trypanocides with the Trypanosoma brucei P2 Aminopurine Transporter

I. Gilbert, M. Barrett, R. Brun, 2005, Antimicrobial Agents and Chemotherapy.

An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes.

I. Gilbert, A. Fairlamb, M. Barrett, 1998, Bioorganic & medicinal chemistry letters.

Synthesis of β‐Keto and α,β‐Unsaturated N‐ Acetylcysteamine Thioesters.

I. Gilbert, J. Staunton, T. J. Simpson, 1995 .

Development of Chemical Proteomics for the Folateome and Analysis of the Kinetoplastid Folateome

Michael D. Urbaniak, G. Drewes, Markus Boesche, 2018, ACS infectious diseases.

Acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase.

G. F. Ruda, I. Gilbert, A. Schipani, 2006, Journal of medicinal chemistry.

Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei

S. Norval, Frederick R. C. Simeons, L. Stojanovski, 2015, Journal of medicinal chemistry.

Drug Discovery for Neglected Diseases: Molecular Target-Based and Phenotypic Approaches

Ian H. Gilbert, I. Gilbert, 2013, Journal of medicinal chemistry.

Dihydrofolate reductase: A potential drug target in trypanosomes and leishmania

Ian H. Gilbert, Janet M. Thornton, Roman A. Laskowski, 1998, J. Comput. Aided Mol. Des..

Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis

Peter G. Dodd, Frederick R. C. Simeons, L. Stojanovski, 2021, Journal of medicinal chemistry.

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition

Juan A. Bueren-Calabuig, David W. Gray, Frederick R. C. Simeons, 2019, Proceedings of the National Academy of Sciences.

Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis

David W. Gray, A. Hill, G. Drewes, 2018, Journal of medicinal chemistry.

N-Myristoyltransferase inhibitors as new leads to treat sleeping sickness

Ian H. Gilbert, Chidochangu P. Mpamhanga, Michael Hodgkinson, 2010, Nature.

Design and synthesis of lipophilic phosphoramidate d4T-MP prodrugs expressing high potency against HIV in cell culture: structural determinants for in vitro activity and QSAR.

I. Gilbert, E. De Clercq, J. Balzarini, 1999, Journal of medicinal chemistry.

Synthesis and Evaluation of α-Thymidine Analogues as Novel Antimalarials

K. Read, I. Gilbert, K. Wilson, 2012, Journal of medicinal chemistry.

Design and synthesis of bio-isosteres of thymidine triphosphate.

I. Gilbert, J. Balzarini, A. Goldring, 1998, Bioorganic & medicinal chemistry letters.

Synthesis and Biological Evaluation of Phosphate Prodrugs of 4-Phospho-d -erythronohydroxamic Acid, an Inhibitor of 6-Phosphogluconate Dehydrogenase

G. F. Ruda, I. Gilbert, V. Alibu, 2007, ChemMedChem.

Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase.

G. F. Ruda, I. Gilbert, D. González-Pacanowska, 2010, European journal of medicinal chemistry.

Design, synthesis and evaluation of novel uracil amino acid conjugates for the inhibition of Trypanosoma cruzi dUTPase.

I. Gilbert, A. Schipani, R. Brun, 2006, Bioorganic & medicinal chemistry letters.

Lipophilic bioisosteres of nucleoside triphosphates

I. Gilbert, J. Balzarini, N. Mahmood, 1996 .

Isosteres of nucleoside triphosphates

I. Gilbert, J. Balzarini, N. Mahmood, 1996 .

Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library

David W. Gray, S. Norval, L. Stojanovski, 2015, ChemMedChem.

Chemogenomics identifies acetyl-coenzyme A synthetase as a target for malaria treatment and prevention

E. Winzeler, I. Gilbert, M. Llinás, 2021, Cell chemical biology.

β-Branched acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase.

Ian H. Gilbert, Keith S. Wilson, Marcel Kaiser, 2011, Bioorganic & medicinal chemistry.

Whole Organism High-Content Screening by Label-Free, Image-Based Bayesian Classification for Parasitic Diseases

Ian H. Gilbert, Andrew L. Hopkins, Irene Hallyburton, 2012, PLoS neglected tropical diseases.

Application of RNAi to Genomic Drug Target Validation in Schistosomes

Ian M. Carruthers, A. Hopkins, I. Gilbert, 2015, PLoS neglected tropical diseases.

Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi

A. Hill, Frederick R. C. Simeons, L. Stojanovski, 2017, Journal of medicinal chemistry.

Structural basis for the efficient phosphorylation of AZT-MP (3'-azido-3'-deoxythymidine monophosphate) and dGMP by Plasmodium falciparum type I thymidylate kinase.

I. Gilbert, K. Wilson, A. Wilkinson, 2010, The Biochemical journal.

MalDA, Accelerating Malaria Drug Discovery

E. Winzeler, I. Gilbert, K. Chibale, 2021, Trends in parasitology.

Lead Optimization of a Pyrazole Sulfonamide Series of Trypanosoma bruceiN-Myristoyltransferase Inhibitors: Identification and Evaluation of CNS Penetrant Compounds as Potential Treatments for Stage 2 Human African Trypanosomiasis

Stuart P. McElroy, S. Norval, Frederick R. C. Simeons, 2014, Journal of medicinal chemistry.

Handling Uncertainty in Dynamic Models: The Pentose Phosphate Pathway in Trypanosoma brucei

David R. Gilbert, Rainer Breitling, Michael P. Barrett, 2013, PLoS Comput. Biol..

Aryl Phosphoramidates of 5-Phospho Erythronohydroxamic Acid, A New Class of Potent Trypanocidal Compounds

G. F. Ruda, S. Norval, K. Read, 2010, Journal of medicinal chemistry.

Crystal structures of a bacterial 6‐phosphogluconate dehydrogenase reveal aspects of specificity, mechanism and mode of inhibition by analogues of high‐energy reaction intermediates

G. F. Ruda, I. Gilbert, M. Barrett, 2007, The FEBS journal.

6-phosphogluconate dehydrogenase: a target for drugs in African trypanosomes.

I. Gilbert, M. Barrett, C. Dardonville, 2004, Current medicinal chemistry.

Selective inhibition of 6-phosphogluconate dehydrogenase from Trypanosoma brucei

Massimo Bertelli, Eman El-Bastawissy, Michael H. Knaggs, 2001, J. Comput. Aided Mol. Des..

Antitrypanosomal 8-Hydroxy-Naphthyridines Are Chelators of Divalent Transition Metals

S. Norval, I. Gilbert, A. Fairlamb, 2018, Antimicrobial Agents and Chemotherapy.

University of Dundee Anti-trypanosomal 8-hydroxyl naphthyridines are chelators of divalent transition metals

S. Norval, I. Gilbert, A. Fairlamb, 2018 .

N-Myristoyltransferase Is a Cell Wall Target in Aspergillus fumigatus

G. F. Ruda, I. Gilbert, D. V. van Aalten, 2015, ACS chemical biology.

Application of a novel regulatable Cre recombinase system to define the role of liver and gut metabolism in drug oral bioavailability

I. Gilbert, C. Wolf, C. Henderson, 2015, The Biochemical journal.

Improved Tricyclic Inhibitors of Trypanothione Reductase by Screening and Chemical Synthesis

Isabelle R. E. Nett, I. Gilbert, A. Fairlamb, 2009, ChemMedChem.

In vitro cell-free conversion of bacterial recombinant PrP to PrPres as a model for conversion.

I. Gilbert, J. Hope, C. Birkett, 2003, The Journal of general virology.

Molecular dynamics simulations of wild-type and point mutation human prion protein at normal and elevated temperature.

I. Gilbert, I H Gilbert, E el-Bastawissy, 2001, Journal of molecular graphics & modelling.

Screening Congo Red and its analogues for their ability to prevent the formation of PrP-res in scrapie-infected cells.

I. Gilbert, J. Hope, C. Birkett, 2000, The Journal of general virology.

Design, Synthesis, and Evaluation of 5′‐Diphenyl Nucleoside Analogues as Inhibitors of the Plasmodium falciparum dUTPase

I. Gilbert, K. Wilson, J. Brannigan, 2011, ChemMedChem.

Analogues of thiolactomycin as potential anti-malarial and anti-trypanosomal agents.

Colin Berry, Ian H Gilbert, I. Gilbert, 2004, Bioorganic & medicinal chemistry.

Prioritization of Molecular Targets for Antimalarial Drug Discovery

E. Winzeler, I. Gilbert, M. Siegel, 2021, ACS infectious diseases.

Setting Our Sights on Infectious Diseases

John P. Overington, P. Herrling, J. McCarthy, 2019, ACS infectious diseases.

Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.

I. Gilbert, S. Croft, J. Goodman, 1999, Journal of medicinal chemistry.

Thiolactomycin analogues as potential anti-Toxoplasma gondii agents.

I. Gilbert, W. de Souza, G. Atella, 2009, Parasitology international.

Evaluation of three novel azasterols against Toxoplasma gondii.

I. Gilbert, W. de Souza, L. Lemgruber, 2011, Veterinary parasitology.

Validation of N-myristoyltransferase as Potential Chemotherapeutic Target in Mammal-Dwelling Stages of Trypanosoma cruzi

I. Gilbert, I. C. Almeida, Armando Varela-Ramírez, 2016, PLoS neglected tropical diseases.

A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors

S. Norval, Frederick R. C. Simeons, L. Stojanovski, 2018, Journal of medicinal chemistry.

Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode

Stuart P. McElroy, S. Norval, L. Stojanovski, 2015, ChemMedChem.

Design, Synthesis and Biological Evaluation of Novel Inhibitors of Trypanosoma brucei Pteridine Reductase 1

K. Read, I. Gilbert, A. Fairlamb, 2010, ChemMedChem.

Chemical Validation of Methionyl-tRNA Synthetase as a Druggable Target in Leishmania donovani

Ian H Gilbert, Manu De Rycker, Sujatha Manthri, 2017, ACS infectious diseases.

Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis

Michael D. Urbaniak, G. Drewes, Markus Boesche, 2018, Nature.

Chemical Validation of Trypanothione Synthetase

I. Gilbert, A. Fairlamb, L. S. Torrie, 2009, The Journal of Biological Chemistry.

Probing the substrate specificity of Trypanosoma brucei GlcNAc-PI de-N-acetylase with synthetic substrate analogues

Michael D. Urbaniak, I. Gilbert, M. Ferguson, 2014, Organic & biomolecular chemistry.

Target assessment for antiparasitic drug discovery.

I. Gilbert, A. Fairlamb, P. Wyatt, 2007, Trends in parasitology.

A QSAR study investigating the effect of L-alanine ester variation on the anti-HIV activity of some phosphoramidate derivatives of d4T.

I. Gilbert, J. Balzarini, C. Mcguigan, 2000, Bioorganic & medicinal chemistry letters.

Target-based drug discovery for human African trypanosomiasis: selection of molecular target and chemical matter

I. Gilbert, 2013, Parasitology.

Target Validation: Linking Target and Chemical Properties to Desired Product Profile

Ian H Gilbert, Paul G Wyatt, K. Read, 2011, Current topics in medicinal chemistry.

Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors

Stuart P. McElroy, S. Norval, L. Stojanovski, 2017, Journal of medicinal chemistry.

Nitrile reduction in the presence of Boc-protected amino groups by catalytic hydrogenation over palladium-activated Raney-nickel.

I. Gilbert, B. Klenke, 2001, The Journal of organic chemistry.

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Ian H. Gilbert, Irene Hallyburton, Alan H. Fairlamb, 2011, Journal of medicinal chemistry.

Validation of Plasmodium falciparum dUTPase as the target of 5′-tritylated deoxyuridine analogues with anti-malarial activity

I. Gilbert, S. Müller, D. González-Pacanowska, 2019, Malaria Journal.

Site-directed mutagenesis provides insights into the selective binding of trityl derivatives to Plasmodium falciparum dUTPase.

G. F. Ruda, I. Gilbert, A. E. Vidal, 2011, European journal of medicinal chemistry.

Investigation of Trypanothione Reductase as a Drug Target in Trypanosoma brucei

Stuart P. McElroy, I. Gilbert, A. Fairlamb, 2009, ChemMedChem.

DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis

I. Gilbert, V. Yardley, B. Nare, 2021, Journal of medicinal chemistry.

Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor

Maria F. Sassano, A. Hopkins, Xi-Ping Huang, 2013, ACS medicinal chemistry letters.

Clinical and Genomic Evolution of Carbapenem-Resistant Klebsiella pneumoniae Bloodstream Infections over Two Time Periods at a Tertiary Care Hospital in South India: A Prospective Cohort Study

I. Gilbert, B. George, V. Mathews, 2023, Infectious Diseases and Therapy.

In Vitro Activity of Two Cefepime-Based Novel Combinations, Cefepime/Taniborbactam and Cefepime/Zidebactam, against Carbapenemase-Expressing Enterobacterales Collected in India

I. Gilbert, A. Mutreja, B. Parcell, 2023, Microbiology spectrum.

Ligand binding: evaluating the contribution of the water molecules network using the Fragment Molecular Orbital method

Ian H. Gilbert, Fabio Zuccotto, Paul G. Wyatt, 2021, Journal of Computer-Aided Molecular Design.

Compounds enhancing human sperm motility identified using a high-throughput phenotypic screening platform

J. Swedlow, K. Read, I. Gilbert, 2021, bioRxiv.

Sperm Toolbox – A selection of small molecules to study human spermatozoa

J. Swedlow, K. Read, I. Gilbert, 2023, bioRxiv.

Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488

S. Norval, K. Read, I. Gilbert, 2011, ChemMedChem.

Antiplasmodial activity of a series of 1,3,5-triazine-substituted polyamines.

I. Gilbert, M. Barrett, R. Brun, 2003, The Journal of antimicrobial chemotherapy.

Fragment library design, synthesis and expansion: nurturing a synthesis and training platform.

Peter C Ray, Michael Kiczun, Margaret Huggett, 2017, Drug discovery today.

Mycobacterium tuberculosis Phe-tRNA synthetase: structural insights into tRNA recognition and aminoacylation

I. Gilbert, A. Joachimiak, J. Wower, 2021, Nucleic acids research.

Design and Synthesis of Covalent Inhibitors of FabA

David W. Gray, I. Gilbert, Nadine Homeyer, 2023, ACS omega.

SophosQM: Accurate Binding Affinity Prediction in Compound Optimization

I. Gilbert, R. Guareschi, F. Zuccotto, 2023, ACS omega.

Lead optimization of a pyrazole sulfonamide series of trypanosoma brucei N myristoyltransferase inhibitors

Stuart P. McElroy, S. Norval, Frederick R. C. Simeons, 2014 .

Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis

E. Winzeler, S. Meister, J. Rayner, 2016, Nature.

Exploring the Trypanosoma brucei Hsp83 Potential as a Target for Structure Guided Drug Design

I. Gilbert, M. Ferguson, A. Wernimont, 2013, PLoS neglected tropical diseases.

Perspective on Schistosomiasis Drug Discovery: Highlights from a Schistosomiasis Drug Discovery Workshop at Wellcome Collection, London, September 2022

K. Read, I. Gilbert, N. Lo, 2023, ACS infectious diseases.

Validation of Plasmodium falciparum dUTPase as the target of 5′-tritylated deoxyuridine analogues with anti-malarial activity

I. Gilbert, S. Müller, D. González-Pacanowska, 2019, Malaria Journal.

Bespoke Drug Discovery Training for Low-Middle Income Countries

K. Read, I. Gilbert, Lauren A. Webster, 2023, ACS Medicinal Chemistry Letters.

Screening a protein kinase inhibitor library against Plasmodium falciparum

I. Gilbert, A. Fairlamb, P. Wyatt, 2017, Malaria Journal.

Discovery of an Allosteric Binding Site in Kinetoplastid Methionyl-tRNA Synthetase

David W. Gray, I. Gilbert, A. Fairlamb, 2020, ACS infectious diseases.

Design, Synthesis and Biological Evaluation of Trypanosoma brucei Trypanothione Synthetase Inhibitors

K. Read, I. Gilbert, A. Fairlamb, 2011, ChemMedChem.

Finding new hits in neglected disease projects: target or phenotypic based screening?

Ian H Gilbert, Didier Leroy, I. Gilbert, 2011, Current topics in medicinal chemistry.

Sperm Toolbox – A selection of small molecules to study human spermatozoa

J. Swedlow, K. Read, I. Gilbert, 2023, bioRxiv.

The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.

I. Gilbert, F. Zuccotto, R. Brun, 1999, Bioorganic & medicinal chemistry letters.

Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors.

Peter G. Dodd, Frederick R. C. Simeons, L. Stojanovski, 2023, Journal of medicinal chemistry.

Author Correction: Anti-trypanosomatid drug discovery: progress and challenges

K. Read, I. Gilbert, D. Horn, 2022, Nature Reviews Microbiology.

Development of a 2,4-Diaminothiazole Series for the Treatment of Human African Trypanosomiasis Highlights the Importance of Static–Cidal Screening of Analogues

S. Norval, Frederick R. C. Simeons, L. Stojanovski, 2023, Journal of Medicinal Chemistry.

Identification of inhibitors of an unconventional Trypanosoma brucei kinetochore kinase

David W. Gray, I. Gilbert, D. Robinson, 2019, PloS one.

Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.

Ian H. Gilbert, Jonathan M. Goodman, I. Gilbert, 1999, Journal of medicinal chemistry.

A platform for target prediction of phenotypic screening hit molecules

Bernardo Ochoa-Montaño, Kathrin Heikamp, Tom L Blundell, 2019, Journal of molecular graphics & modelling.

Author Correction: Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis

Michael D. Urbaniak, David W. Gray, G. Drewes, 2023, Nature.

Setting Our Sights on Infectious Diseases

John P. Overington, P. Herrling, J. McCarthy, 2019, ACS infectious diseases.

Synthesis and testing of peptides for anti-prion activity.

I. Gilbert, David R. Brown, C. Boussard, 2008, European journal of medicinal chemistry.

Fragment library design, synthesis and expansion: nurturing a synthesis and training platform.

I. Gilbert, P. Wyatt, Andrew S. T. Lim, 2017, Drug discovery today.

Comparison of a High-Throughput High-Content Intracellular Leishmania donovani Assay with an Axenic Amastigote Assay

David W. Gray, S. Cameron, I. Gilbert, 2013, Antimicrobial Agents and Chemotherapy.

Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis† †Electronic supplementary information (ESI) available. See DOI: 10.1039/d0md00203h

S. Norval, Frederick R. C. Simeons, L. Stojanovski, 2020, RSC medicinal chemistry.

Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis

Michael D. Urbaniak, David W. Gray, G. Drewes, 2018, Nature.

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

Mark C. Field, David W. Gray, K. Read, 2017, Nature Reviews Microbiology.

Synthesis and Testing of 5-Benzyl-2,4-diaminopyrimidines as Potential Inhibitors of Leishmanial and Trypanosomal Dihydrofolate Reductase

I. Gilbert, R. Brun, S. Chowdhury, 2002, Journal of enzyme inhibition and medicinal chemistry.

Author Correction: Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

Mark C. Field, David W. Gray, K. Read, 2018, Nature Reviews Microbiology.

Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase.

G. F. Ruda, I. Gilbert, D. González-Pacanowska, 2010, European journal of medicinal chemistry.

Clinical and veterinary trypanocidal benzoxaboroles target CPSF3

Mark C. Field, I. Gilbert, D. Horn, 2018, Proceedings of the National Academy of Sciences.