K. White

发表

Introduction of lipidization–cationization motifs affords systemically bioavailable neuropeptide Y and neurotensin analogs with anticonvulsant activities

E. Scholl, G. Bulaj, H. White, 2010, Journal of peptide science : an official publication of the European Peptide Society.

SGLT2 inhibitors or GLP-1 receptor agonists as second-line therapy in type 2 diabetes: patient selection and perspectives

C. McAdam-Marx, K. White, Holly E. Gurgle, 2016, Vascular health and risk management.

Nitroheterocyclic drugs cure experimental Trypanosoma cruzi infections more effectively in the chronic stage than in the acute stage

David M. Shackleford, K. Read, E. Chatelain, 2016, Scientific Reports.

Antitrypanosomal Activity of Fexinidazole Metabolites, Potential New Drug Candidates for Chagas Disease

David M. Shackleford, E. Chatelain, S. Charman, 2014, Antimicrobial Agents and Chemotherapy.

An in vitro toolbox to accelerate anti-malarial drug discovery and development

David M. Shackleford, Dennis A. Smith, S. Charman, 2020, Malaria Journal.

3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis.

J. Baell, V. Avery, S. Charman, 2013, European journal of medicinal chemistry.

Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity

P. Rathod, John White, M. Phillips, 2016, Journal of medicinal chemistry.

Two Analogues of Fenarimol Show Curative Activity in an Experimental Model of Chagas Disease

David M. Shackleford, M. J. Abbott, Paul W. Alexander, 2013, Journal of medicinal chemistry.

Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials.

J. Gut, P. Rosenthal, R. Payne, 2019, Journal of medicinal chemistry.

Orally Bioavailable 6-Chloro-7-methoxy-4(1H)-quinolones Efficacious against Multiple Stages of Plasmodium

David M. Shackleford, W. Guida, D. Kyle, 2014, Journal of medicinal chemistry.

Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines.

K. Chibale, M. Witty, S. Charman, 2012, Journal of medicinal chemistry.

Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones

David M. Shackleford, R. Guy, S. Charman, 2020, Malaria journal.

A Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Improved Drug-like Properties for Treatment and Prevention of Malaria.

David M. Shackleford, R. Price, P. Rathod, 2016, ACS infectious diseases.

Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).

David M. Shackleford, J. Chollet, S. Charman, 2017, Journal of medicinal chemistry.

In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models

David M. Shackleford, S. Charman, R. Brun, 2013, Drug design, development and therapy.

Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials.

David M. Shackleford, Laura M Sanz, K. Dechering, 2021, Journal of medicinal chemistry.

Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities.

E. Scholl, G. Bulaj, H. White, 2008, Journal of medicinal chemistry.

Repositioning and Characterization of 1-(Pyridin-4-yl)pyrrolidin-2-one Derivatives as Plasmodium Cytoplasmic Prolyl-tRNA Synthetase Inhibitors

David M. Shackleford, D. Fidock, Laura M Sanz, 2021, ACS infectious diseases.

Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.

E. Winzeler, S. Meister, K. Chibale, 2016, Journal of medicinal chemistry.

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1.

K. Chibale, Dale Taylor, M. Witty, 2014, Journal of medicinal chemistry.

Progress in antischistosomal N,N'-diaryl urea SAR.

David M. Shackleford, J. Keiser, S. Charman, 2017, Bioorganic & medicinal chemistry letters.

Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.

David M. Shackleford, Paul W. Alexander, E. Chatelain, 2013, Bioorganic & medicinal chemistry.

Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.

M. J. Abbott, Paul W. Alexander, E. Chatelain, 2012, Journal of medicinal chemistry.

Pharmacological Characterization, Structural Studies, and In Vivo Activities of Anti-Chagas Disease Lead Compounds Derived from Tipifarnib

David M. Shackleford, M. Gelb, F. Buckner, 2012, Antimicrobial Agents and Chemotherapy.

Analgesic neuropeptide W suppresses seizures in the brain revealed by rational repositioning and peptide engineering.

G. Bulaj, H. White, B. R. Green, 2011, ACS chemical neuroscience.

Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity.

K. Chibale, M. Witty, S. Charman, 2013, Journal of medicinal chemistry.

3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential.

David M. Shackleford, K. Chibale, M. Witty, 2012, Journal of medicinal chemistry.

ELQ-300 Prodrugs for Enhanced Delivery and Single-Dose Cure of Malaria

David M. Shackleford, Galen P. Miley, M. Mather, 2015, Antimicrobial Agents and Chemotherapy.

Discovery, Synthesis, and Optimization of Antimalarial 4(1H)-Quinolone-3-Diarylethers

Galen P. Miley, M. Mather, A. Vaidya, 2014, Journal of medicinal chemistry.

Isoxazolopyrimidine-Based Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Antimalarial Activity

David M. Shackleford, P. Rathod, John White, 2018, ACS omega.

Structure–Activity Relationship Studies of Pyrrolone Antimalarial Agents

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

Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice.

David M. Shackleford, Pradipsinh K Rathod, Karen L White, 2009, Journal of medicinal chemistry.

Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.

David M. Shackleford, Susan A Charman, Pradipsinh K Rathod, 2011, Journal of medicinal chemistry.

2,4-Diaminothienopyrimidines as orally active antimalarial agents.

K. Chibale, Dale Taylor, M. Witty, 2014, Journal of medicinal chemistry.

Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.

David M. Shackleford, Francisco-Javier Gamo, Xiaoyi Deng, 2011, Journal of medicinal chemistry.

Novel orally active antimalarial thiazoles.

K. Chibale, M. Witty, S. Charman, 2011, Journal of medicinal chemistry.

Pyridyl benzamides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei.

Christel A. S. Bergström, J. Baell, V. Avery, 2014, Journal of medicinal chemistry.

Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines.

David M. Shackleford, J. Baell, V. Avery, 2021, Journal of medicinal chemistry.

Novel inhibitors of Plasmodium falciparum based on 2,5-disubstituted furans.

S. Charman, E. Ryan, L. Dias, 2017, European journal of medicinal chemistry.

Evaluation of robenidine analog NCL195 as a novel broad-spectrum antibacterial agent

Sanjay Garg, Adam McCluskey, Karen White, 2017, PloS one.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria

R. Price, K. Chibale, Dale Taylor, 2018, Antimicrobial Agents and Chemotherapy.

Glycine Loss and Maillard Browning as Related to the Glass Transition in a Model Food System

L. Bell, D. Touma, K. White, 2006 .

Thiamin stability in solids as affected by the glass transition

L. Bell, K. White, 2000 .

Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.

K. Read, W. Denny, A. M. Thompson, 2020, European journal of medicinal chemistry.

Antitrypanosomal activity of fexinidazole metabolites, potential new drug candidates 1

Susan, E. Chatelain, A. Talvani, 2014 .

Lymphatic Transport of Methylnortestosterone Undecanoate (MU) and the Bioavailability of Methylnortestosterone Are Highly Sensitive to the Mass of Coadministered Lipid after Oral Administration of MU

Christopher J H Porter, Karen L White, G. Edwards, 2009, Journal of Pharmacology and Experimental Therapeutics.

Mannosylated liposomes as antigen delivery vehicles for targeting to dendritic cells

R. Furneaux, P. Tyler, T. Rades, 2006, The Journal of pharmacy and pharmacology.

Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth

Nghi Nguyen, Thomas S. Peat, Olan Dolezal, 2018, Nature.

Discovery of Acylsulfonohydrazide-Derived Lysine Acetyltransferase (KAT6A) Inhibitors as Potent Senescence-Inducing Anti-Cancer Agents.

Jayme L. Dahlin, David M. Shackleford, J. Baell, 2020, Journal of medicinal chemistry.

A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria

Farah El Mazouni, T. Laird, P. Rathod, 2015, Science Translational Medicine.

Preclinical anticancer activity of cryptophycin-8.

P. Lorusso, F. Valeriote, T. Corbett, 1996, Journal of experimental therapeutics & oncology.

Quinolone-3-Diarylethers: A New Class of Antimalarial Drug

Yuexin Li, David M. Shackleford, Susan A Charman, 2013, Science Translational Medicine.

Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria

Christian Scheurer, Lukas Stingelin, David M. Shackleford, 2011, Proceedings of the National Academy of Sciences.

Preclinical Comparison of Mechanistically Different Antiseizure, Antinociceptive, and/or Antidepressant Drugs in a Battery of Rodent Models of Nociceptive and Neuropathic Pain

K. Wilcox, Timothy H. Pruess, K. White, 2017, Neurochemical Research.

Quinolone-3-Diarylethers : A new class of drugs for a new era of malaria eradication

David M. Shackleford, R. Price, M. Mather, 2014 .

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase

David M. Shackleford, G. Drewes, M. Bantscheff, 2017, Science Translational Medicine.

Antimalarial activity of pyrroloiminoquinones from the Australian marine sponge Zyzzya sp.

David M. Shackleford, V. Avery, S. Charman, 2012, Journal of medicinal chemistry.

Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target

Yongyuth Yuthavong, Sumalee Kamchonwongpaisan, Jarunee Vanichtanankul, 2012, Proceedings of the National Academy of Sciences.

Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978)

David M. Shackleford, J. Keiser, Jeremy O. Jones, 2016, Journal of medicinal chemistry.

Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride.

David M. Shackleford, M. Ranson, S. Charman, 2021, Bioorganic & medicinal chemistry.

Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth

A. Strasser, G. Smyth, J. Baell, 2018, Nature.

Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures.

F. Diederich, R. Aponte, P. Chaiyen, 2017, Journal of medicinal chemistry.

Selection and optimization of hits from a high-throughput phenotypic screen against Trypanosoma cruzi.

M. J. Abbott, Paul W. Alexander, S. Cornwall, 2013, Future medicinal chemistry.

The role of thioredoxin reductase 1 in melanoma metabolism and metastasis

P. Cassidy, S. Leachman, S. Florell, 2015, Pigment cell & melanoma research.

Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles

Julie Clark, George Papadatos, Jeremy N. Burrows, 2016, ACS central science.

6-Arylpyrazine-2-carboxamides: A New Core for Trypanosoma brucei Inhibitors.

J. Baell, V. Avery, S. Charman, 2015, Journal of medicinal chemistry.

Extraction of Coal Tar Pitch Using a Mixture of Compressed CO2 and Toluene

G. Kimber, K. White, B. Knutson, 1999 .

Discovery of benzoylsulfonohydrazides as potent inhibitors of the histone acetyltransferase KAT6A.

Jayme L. Dahlin, J. Baell, M. Walters, 2019, Journal of medicinal chemistry.

Using Human Plasma as an Assay Medium in Caco-2 Studies Improves Mass Balance for Lipophilic Compounds

David M. Shackleford, S. Charman, Nada Abla, 2018, Pharmaceutical Research.

Structure-Activity Relationship of Antischistosomal Ozonide Carboxylic Acids.

David M. Shackleford, J. Keiser, S. Charman, 2020, Journal of medicinal chemistry.

Lead optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series for the treatment of Malaria.

David M. Shackleford, P. Rathod, John White, 2020, Journal of medicinal chemistry.

Potent in Vitro and in Vivo Antimalarials

J. Gut, R. Payne, N. Hunt, 2019 .

Maillard reaction in glassy low-moisture solids as affected by buffer type and concentration

L. Bell, K. White, Yin-Hui Chen, 1998 .

Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice

David M. Shackleford, S. Norval, K. Read, 2011, Malaria Journal.

Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.

David M. Shackleford, E. Winzeler, P. Rathod, 2021, Journal of medicinal chemistry.

Gas antisolvent fractionation of semicrystalline and amorphous poly(lactic acid) using compressed CO2

B. L. Knutson, G. Bothun, K. White, 2002 .

Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Apicomplexan Parasites In Vitro and in a P. falciparum Humanized NOD-scid IL2Rγnull Mouse Model of Malaria

Christopher J. Tonkin, A. Cowman, F. Gamo, 2018, Antimicrobial Agents and Chemotherapy.

Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.

Chin Wee Tan, Dharmesh D. Bhuva, Eric C Greenwald, 2023, Cell chemical biology.

Recurrent Achromobacter piechaudiiBacteremia in a Patient with Hematological Malignancy

M. Peel, R. Clark, K. White, 2001, Journal of Clinical Microbiology.

Abstract 5371: PRMT5 inhibitors as novel treatment for cancers

T. Peat, P. Pilling, S. Jane, 2015 .

SAR of a new antischistosomal urea carboxylic acid.

David M. Shackleford, J. Keiser, S. Charman, 2018, Bioorganic & medicinal chemistry letters.