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DS86760016, a Leucyl-tRNA Synthetase Inhibitor with Activity against Pseudomonas aeruginosa

Antimicrobial agents and chemotherapy, 2019-04, Vol.63 (4)

2019

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Correlation of in vitro and in vivo plasma protein binding using ultracentrifugation and UPLC-tandem mass spectrometry

Analyst (London), 2013-10, Vol.138 (20), p.6106-6116

2013

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Synthesis and evaluation of thiomannosides, potent and orally active FimH inhibitors

Bioorganic & medicinal chemistry letters, 2018-09, Vol.28 (17), p.2993-2997

2018

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Preclinical drug metabolism and pharmacokinetics of salinomycin, a potential candidate for targeting human cancer stem cells

Chemico-biological interactions, 2015-10, Vol.240, p.146-152

2015

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Candidate Selection and Preclinical Evaluation of N-tert-Butyl Isoquine (GSK369796), An Affordable and Effective 4-Aminoquinoline Antimalarial for the 21st Century

Journal of medicinal chemistry, 2009-03, Vol.52 (5), p.1408-1415

2009

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Pharmacokinetics and brain penetration of casopitant, a potent and selective neurokinin-1 receptor antagonist, in the ferret

Drug metabolism and disposition, 2008-09, Vol.36 (9), p.1846

2008

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Characterization and inhibition of a cholecystokinin-inactivating serine peptidase

Nature (London), 1996-04, Vol.380 (6573), p.403-409

1996

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In Vitro and In Vivo Activities of DS86760016, a Novel Leucyl-tRNA Synthetase Inhibitor for Gram-Negative Pathogens

Antimicrobial agents and chemotherapy, 2018-04, Vol.62 (4)

2018

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Novel FtsZ inhibitor with potent activity against Staphylococcus aureus

Journal of antimicrobial chemotherapy, 2021-10, Vol.76 (11), p.2867-2874

2021

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Inhibitors of Tripeptidyl Peptidase II. 3. Derivation of Butabindide by Successive Structure Optimizations Leading to a Potential General Approach to Designing Exopeptidase Inhibitors

Journal of medicinal chemistry, 2005-11, Vol.48 (23), p.7333-7342

2005

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Correlation of in vitro and in vivo plasma protein binding using ultracentrifugation and UPLC-tandem mass spectrometryElectronic supplementary information (ESI) available. See DOI: 10.1039/c3an01116j

2013-09

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3-(1,1-Dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, Potent Inhibitors of Hepatitis C Virus RNA-Dependent RNA Polymerase

Journal of medicinal chemistry, 2006-02, Vol.49 (3), p.971-983

2006

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Correlation of in vitroand in vivoplasma protein binding using ultracentrifugation and UPLC-tandem mass spectrometry

Analyst (London), 2013-09, Vol.138 (20), p.6106-6116

2013

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Abstract 1560: Orally bioavailable macrocycles that target cyclins A and B RxL motifs cause tumor regression in xenograft models and in vitro show activity across multiple cancer types

Cancer research (Chicago, Ill.), 2023-04, Vol.83 (7_Supplement), p.1560-1560

2023

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Bromobenzene 3,4-Oxide Alkylates Histidine and Lysine Side Chains of Rat Liver Proteins in Vivo

Chemical research in toxicology, 1995-07, Vol.8 (5), p.729-735

1995

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Inhibitors of Tripeptidyl Peptidase II. 2. Generation of the First Novel Lead Inhibitor of Cholecystokinin-8-Inactivating Peptidase: A Strategy for the Design of Peptidase Inhibitors

Journal of medicinal chemistry, 2000-02, Vol.43 (4), p.664-674

2000

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Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding

Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (6), p.1694-1697

2009

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Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase

Bioorganic & medicinal chemistry letters, 2009-08, Vol.19 (15), p.4350-4353

2009

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Preclinical Drug Metabolism and Pharmacokinetic Evaluation of GW844520, A Novel Anti-Malarial Mitochondrial Electron Transport Inhibitor

Journal of pharmaceutical sciences, 2006-12, Vol.95 (12), p.2657-2672

2006

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Effects of Steric Bulk and Conformational Rigidity on Fatty Acid Omega Hydroxylation by a Cytochrome P450 4A1 Fusion Protein

Archives of biochemistry and biophysics, 1996-10, Vol.334 (1), p.59-66

1996

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Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: Potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties

Bioorganic & medicinal chemistry letters, 2010-08, Vol.20 (15), p.4587-4592

2010

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Active Site Structure and Substrate Specificity of Cytochrome P450 4A1: Steric Control of Ligand Approach Perpendicular to Heme Plane

Biochemical and biophysical research communications, 1996-02, Vol.219 (2), p.445-449

1996

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Comparative preclinical drug metabolism and pharmacokinetic evaluation of novel 4-aminoquinoline anti-malarials

Journal of pharmaceutical sciences, 2009-01, Vol.98 (1), p.362-377

2009

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Corrigendum to “Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding” [Bioorg. Med. Chem. Lett. 19 (2009) 1694]

Bioorganic & medicinal chemistry letters, 2009-05, Vol.19 (9), p.2604-2604

2009

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DS86760016, a Leucyl-tRNA Synthetase Inhibitor with Activity against Pseudomonas aeruginosa

Correlation of in vitro and in vivo plasma protein binding using ultracentrifugation and UPLC-tandem mass spectrometry

Synthesis and evaluation of thiomannosides, potent and orally active FimH inhibitors

Preclinical drug metabolism and pharmacokinetics of salinomycin, a potential candidate for targeting human cancer stem cells

Candidate Selection and Preclinical Evaluation of N-tert-Butyl Isoquine (GSK369796), An Affordable and Effective 4-Aminoquinoline Antimalarial for the 21st Century

Synthesis, Antimalarial Activity, and Preclinical Pharmacology of a Novel Series of 4′-Fluoro and 4′-Chloro Analogues of Amodiaquine. Identification of a Suitable “Back-Up” Compound for N-tert-Butyl Isoquine

Pharmacokinetics and brain penetration of casopitant, a potent and selective neurokinin-1 receptor antagonist, in the ferret

Characterization and inhibition of a cholecystokinin-inactivating serine peptidase

In Vitro and In Vivo Activities of DS86760016, a Novel Leucyl-tRNA Synthetase Inhibitor for Gram-Negative Pathogens

Novel FtsZ inhibitor with potent activity against Staphylococcus aureus

Inhibitors of Tripeptidyl Peptidase II. 3. Derivation of Butabindide by Successive Structure Optimizations Leading to a Potential General Approach to Designing Exopeptidase Inhibitors

Correlation of in vitro and in vivo plasma protein binding using ultracentrifugation and UPLC-tandem mass spectrometryElectronic supplementary information (ESI) available. See DOI: 10.1039/c3an01116j

3-(1,1-Dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, Potent Inhibitors of Hepatitis C Virus RNA-Dependent RNA Polymerase

Correlation of in vitroand in vivoplasma protein binding using ultracentrifugation and UPLC-tandem mass spectrometry

Abstract 1560: Orally bioavailable macrocycles that target cyclins A and B RxL motifs cause tumor regression in xenograft models and in vitro show activity across multiple cancer types

Bromobenzene 3,4-Oxide Alkylates Histidine and Lysine Side Chains of Rat Liver Proteins in Vivo

Inhibitors of Tripeptidyl Peptidase II. 2. Generation of the First Novel Lead Inhibitor of Cholecystokinin-8-Inactivating Peptidase: A Strategy for the Design of Peptidase Inhibitors

Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding

Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase

Preclinical Drug Metabolism and Pharmacokinetic Evaluation of GW844520, A Novel Anti-Malarial Mitochondrial Electron Transport Inhibitor

Effects of Steric Bulk and Conformational Rigidity on Fatty Acid Omega Hydroxylation by a Cytochrome P450 4A1 Fusion Protein

Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: Potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties

Active Site Structure and Substrate Specificity of Cytochrome P450 4A1: Steric Control of Ligand Approach Perpendicular to Heme Plane

Comparative preclinical drug metabolism and pharmacokinetic evaluation of novel 4-aminoquinoline anti-malarials

Corrigendum to “Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding” [Bioorg. Med. Chem. Lett. 19 (2009) 1694]

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