L. Street

发表

L‐694,247: a potent 5‐HT1D receptor agonist

D. Middlemiss, V. Matassa, R. Hargreaves, 1993, British journal of pharmacology.

Selective, Orally Active γ-Aminobutyric AcidA α5 Receptor Inverse Agonists as Cognition Enhancers

Desmond O'Connor, G. Dawson, J. Atack, 2004 .

Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization.

C. Harris, K. Chibale, D. Warner, 2015, Bioorganic & medicinal chemistry.

Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist

Sandra M. Sanabria-Bohórquez, G. Bormans, K. Van Laere, 2011, Journal of psychopharmacology.

Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies

G. Drewes, C. Harris, Markus Boesche, 2017, Journal of medicinal chemistry.

Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.

Paul W Smith, K. Chibale, Dale Taylor, 2015, 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.

Potentiation of rifampin activity in a mouse model of tuberculosis by activation of host transcription factor EB

A. Ballabio, K. Chibale, J. Camardo, 2020, PLoS pathogens.

Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines.

K. Chibale, Dale Taylor, M. Witty, 2015, Journal of medicinal chemistry.

Lerisetron Analogues with Antimalarial Properties: Synthesis, Structure–Activity Relationship Studies, and Biological Assessment

C. Eyermann, K. Chibale, Dale Taylor, 2020, ACS omega.

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.

A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.

E. Winzeler, S. Meister, K. Chibale, 2015, 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.

Imidazo[1,2-b][1,2,4]triazines as α2/α3 subtype selective GABAA agonists for the treatment of anxiety

S. Tye, A. Pike, J. Atack, 2006 .

Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials

K. Chibale, D. Mancama, D. Leroy, 2018, The Journal of antimicrobial chemotherapy.

TPA023 [7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an Agonist Selective for α2- and α3-Containing GABAA Receptors, Is a Nonsedating Anxiolytic in Rodents and Primates

G. Dawson, S. Tye, R. Mckernan, 2006, Journal of Pharmacology and Experimental Therapeutics.

Synthesis and biological evaluation of aryl-oxadiazoles as inhibitors of Mycobacterium tuberculosis

A. Korkegian, K. Chibale, T. Parish, 2018, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.

G. Dawson, R. Mckernan, A. Pike, 2004, Journal of medicinal chemistry.

The Pharmacology and Mechanisms of Action of Rizatriptan

R. Hargreaves, G. Seabrook, M. Beer, 2000 .

Synthesis of 3,5-disubstituted 1-azabicyclic systems: Intermediates for novel muscarinic ligands

R. Snow, L. Street, 1989 .

Benzotriazinone and benzopyrimidinone derivatives as potent positive allosteric AMPA receptor modulators.

Steven W. Johnson, G. Rogers, Sheng Zhong, 2011, Bioorganic & medicinal chemistry letters.

Synthesis and muscarinic activity of quinuclidinyl- and (1-azanorbornyl)pyrazine derivatives.

T. Willson, S. Freedman, S. Patel, 1992, Journal of medicinal chemistry.

2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.

Karen S. Curley, R. Mckernan, J. Atack, 2004, Bioorganic & medicinal chemistry letters.

Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.

A. Pike, J. Atack, K. Wafford, 2006, Bioorganic & medicinal chemistry letters.

Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.

K. Chibale, Dale Taylor, K. Wicht, 2018, Journal of medicinal chemistry.

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.

Benzobistriazinones and related heterocyclic ring systems as potent, orally bioavailable positive allosteric AMPA receptor modulators.

Steven A. Johnson, Sheng Zhong, R. Mueller, 2011, Bioorganic & medicinal chemistry letters.

3-Phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and Analogues: High-Affinity γ-Aminobutyric Acid-A Benzodiazepine Receptor Ligands with α2, α3, and α5-Subtype Binding Selectivity over α1

G. Dawson, P. Leeson, R. Mckernan, 2004 .

3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.

G. Dawson, P. Leeson, R. Mckernan, 2004, Journal of medicinal chemistry.

Imidazo[1,2-a]pyrimidines as Functionally Selective and Orally Bioavailable GABAAα2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders

Joanna Stanley, A. Pike, J. Atack, 2006 .

Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors.

S. Freedman, L. Street, A. Macleod, 1990, Journal of medicinal chemistry.

Synthesis of cyclic ethers from copper carbenoids by formation and rearrangement of oxonium ylides

J. S. Clark, L. Street, S. A. Krowiak, 1993 .

Rearrangement of ammonium ylides produced by intramolecular reaction of catalytically generated metal carbenoids. Part 1. Synthesis of cyclic amines

Michael D. Goldsmith, J. S. Clark, L. Street, 2001 .

Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.

V. Matassa, M. Beer, J. Stanton, 1997, Journal of medicinal chemistry.

3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.

V. Matassa, M. Beer, J. Stanton, 1997, Journal of medicinal chemistry.

2,4-Diaminothienopyrimidines as orally active antimalarial agents.

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

Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors.

D. Middlemiss, V. Matassa, M. Beer, 1993, Journal of medicinal chemistry.

Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.

V. Matassa, M. Beer, J. Stanton, 1999, Journal of medicinal chemistry.

Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.

M. Beer, A. Reeve, L. Street, 1995, Journal of medicinal chemistry.

Synthesis, biological activity and electrostatic properties of 3-[2-(dimethylamino)ethyl]-5-[(3-amino-1,2,4-thiadiazol-5-yl)methyl]-1H-indole, a novel 5-HT1D receptor agonist.

H. Broughton, V. Matassa, R. Mosley, 1993 .

Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors.

S. Freedman, L. Street, A. Macleod, 1990, Journal of medicinal chemistry.

An Efficient Synthesis of the Indole Acetic Acid Metabolite of MK-0462

Cheng-yi Chen, L. Street, T. Verhoeven, 1996 .

Total synthesis of (±)-β-bulnesene via intramolecular cycloaddition of a 2-substituted 3-oxidopyrylium

S. Bromidge, P. G. Sammes, L. Street, 1985 .

Rapid analogue synthesis of trisubstituted triazolo[4,3-b]pyridazines

I. Collins, L. Street, J. Castro, 2000 .

Pyrazolopyridinones as functionally selective GABAA ligands.

R. Mckernan, J. Atack, K. Wafford, 2005, Bioorganic & medicinal chemistry letters.

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.

Synthesis of (±)-cryptofauronol and related valerane sesquiterpenes via rearrangement of bicyclo[5.3.0]decane precursors

P. G. Sammes, L. Street, R. Whitby, 1986 .

Synthesis, physicochemical and conformational properties of (3R,4R)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane, a novel M1 selective muscarinic partial agonist

R. Hargreaves, S. Freedman, K. Hoogsteen, 1992 .

Synthesis of azabicyclic pyrazine derivatives as muscarinic agonists and the preparation of a chloropyrazine analogue with functional selectivity at sub-types of the muscarinic receptor

A. Reeve, L. Street, J. Saunders, 1991 .

A novel series of non‐quaternary oxadiazoles acting as full agonists at muscarinic receptors

L. Iversen, N. Newberry, J. Maguire, 1990, British journal of pharmacology.

3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.

V. Matassa, M. Beer, J. Stanton, 1999, Journal of medicinal chemistry.

Rearrangement of ammonium ylides produced by intramolecular reaction of catalytically generated metal carbenoids. Part 2. Stereoselective synthesis of bicyclic amines

Michael D. Goldsmith, A. J. Blake, L. Street, 2001 .

Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum

K. Chibale, Xavier C Ding, D. Leroy, 2013, Malaria Journal.

Benzoheterocyclic Oxime Carbamates Active against Mycobacterium tuberculosis: Synthesis, Structure-Activity Relationship, Metabolism, and Biology Triaging.

Paul W Smith, K. Chibale, Dale Taylor, 2021, Journal of medicinal chemistry.

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

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

Evidence for a Significant Role of α3-Containing GABAA Receptors in Mediating the Anxiolytic Effects of Benzodiazepines

G. Dawson, R. Dias, S. Tye, 2005, The Journal of Neuroscience.

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: part 2.

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

Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains.

C. Eyermann, K. Chibale, Dale Taylor, 2018, Journal of medicinal chemistry.

Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model.

K. Chibale, T. Egan, Dale Taylor, 2020, Journal of medicinal chemistry.

7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.

G. Dawson, R. Mckernan, A. Pike, 2005, Journal of medicinal chemistry.

2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure–Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization

K. Read, K. Chibale, T. Ioerger, 2018, ACS infectious diseases.

Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.

S. Tye, A. Pike, J. Atack, 2006, Journal of medicinal chemistry.

The preparation and some reactions of 3-oxidopyrylium

P. G. Sammes, L. Street, P. Sammes, 1983 .

Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria

K. Chibale, Dale Taylor, G. Basarab, 2018, Antimicrobial Agents and Chemotherapy.

Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.

C. Eyermann, K. Chibale, Dale Taylor, 2018, Journal of medicinal chemistry.

Chemoselective cycloadditions of 3,4-dialkoxyfurans and alkyl coumalates. Novel loss of aromaticity of two nonbenzenoid aromatic rings in a mild thermal process

M. Jung, Y. Usui, L. Street, 1986 .

Chemoselective Cycloadditions of 3,4-Dialkoxyfurans and Alkyl Coumalates. Novel Loss of Aromaticity of Two Non-Benzenoid Aromatic Rings in a Mild Thermal Process.

M. Jung, Y. Usui, L. Street, 1987 .

Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour

G. Dawson, J. Atack, C. McCabe, 2004, Neuropharmacology.

Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as α2/α3 subtype selective GABAA agonists for the treatment of anxiety

A. Pike, J. Atack, K. Wafford, 2006 .

2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: Functionally selective GABAA α3-subtype agonists

J. Atack, K. Wafford, L. Street, 2006 .

Imidazo[1,2-a]pyrazin-8-ones, Imidazo[1,2-d][1,2,4]triazin-8-ones and Imidazo[2,1-f][1,2,4]triazine-8-ones as α2/α3 Subtype Selective GABAA Agonists for the Treatment of Anxiety.

A. Pike, J. Atack, K. Wafford, 2006 .

Cell-based medicinal chemistry optimization of high throughput screening hits for orally active antimalarials. Part 2: hits from SoftFocus kinase and other libraries.

K. Chibale, M. Witty, L. Street, 2013, Journal of medicinal chemistry.

Identification of Plasmodium PI4 kinase as target of MMV390048 by chemoproteomics

G. Drewes, M. Bantscheff, K. Chibale, 2014, Malaria Journal.

The synthesis and preclinical evaluation in rhesus monkey of [18F]MK‐6577 and [11C]CMPyPB glycine transporter 1 positron emission tomography radiotracers

Sandra M. Sanabria-Bohórquez, Christine Ryan, Kerry Riffel, 2011, Synapse.

Novel rearragements of 7-oxanorbornene systems

M. Jung, L. Street, 1985 .

Synthetic studies on the avermectins: substituent effects on intramolecular Diels-Alder reactions of N-furfurylacrylamides and further reactions of the cycloadducts

M. Jung, L. Street, 1984 .

Synthetic approach to the ivermectin bottom half using internal cycloadducts of N-furfuryl acrylamides: functionality and optical activity

M. Jung, L. Street, 1988 .

Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABAA receptor α1 subtype

R. Mckernan, P. Whiting, J. Atack, 2000, Nature Neuroscience.

Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1.

A. Pike, H. Burns, T. Hamill, 2010, ACS medicinal chemistry letters.

Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization.

C. Harris, K. Chibale, D. Warner, 2015, Bioorganic & medicinal chemistry.

Intramolecular cycloadditions with oxidopyrylium ylides

L. Street, P. Sammes, 1983 .

Preparation and properties of some phytotoxic 2-benzyloxy-8-oxabicyclo[3.2.1]octane derivatives

L. Street, P. Kirby, P. Sammes, 1983 .

Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.

E. Winzeler, K. Chibale, Dale Taylor, 2021, Journal of medicinal chemistry.