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Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Journal of medicinal chemistry, 2005-07, Vol.48 (15), p.5025-5037

2005

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Mechanism of Inhibition for BMS-791325, a Novel Non-nucleoside Inhibitor of Hepatitis C Virus NS5B Polymerase

The Journal of biological chemistry, 2014-11, Vol.289 (48), p.33456-33468

2014

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Involvement of DPP‐IV catalytic residues in enzyme–saxagliptin complex formation

Protein science, 2008-02, Vol.17 (2), p.240-250

2008

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Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors

Bioorganic & medicinal chemistry letters, 2013-03, Vol.23 (6), p.1622-1625

2013

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Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1

Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.537-541

2011

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Parallel Synthesis of Potent, Pyrazole-Based Inhibitors of Helicobacter pylori Dihydroorotate Dehydrogenase

Journal of medicinal chemistry, 2002-10, Vol.45 (21), p.4669-4678

2002

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NADH Dehydrogenase Defects Confer Isoniazid Resistance and Conditional Lethality in Mycobacterium smegmatis

Journal of Bacteriology, 1998-05, Vol.180 (9), p.2459-2467

1998

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Antisense RNA to ahpC, an oxidative stress defence gene involved in isoniazid resistance, indicates that AhpC of Mycobacterium bovis has virulence properties

Microbiology (Society for General Microbiology), 1998-10, Vol.144 ( Pt 10), p.2687

1998

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Evidence for Isoniazid Oxidation by Oxyferrous Mycobacterial Catalase−Peroxidase

Journal of the American Chemical Society, 1996-11, Vol.118 (45), p.11303-11304

1996

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Discovery of a novel, highly potent and orally bioavailable pyrrolidinone indole series of irreversible Myeloperoxidase (MPO) inhibitors

Biochemical pharmacology, 2023-03, Vol.209, p.115418, Article 115418

2023

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Helicobacter pylori-selective Antibacterials Based on Inhibition of Pyrimidine Biosynthesis

The Journal of biological chemistry, 2000-10, Vol.275 (43), p.33373-33378

2000

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Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO)

Bioorganic & medicinal chemistry, 2020-06, Vol.28 (12), p.115548-115548, Article 115548

2020

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The Role of Mn(II)-Peroxidase Activity of Mycobacterial Catalase-Peroxidase in Activation of the Antibiotic Isoniazid

The Journal of biological chemistry, 1997-04, Vol.272 (14), p.8867-8870

1997

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Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1 H -pyrazol-1-yl)methyl)phosphonate (BMS-820132)

Journal of medicinal chemistry, 2022-03, Vol.65 (5), p.4291-4317

2022

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Purification and Characterization of the Mycobacterium smegmatis Catalase-Peroxidase Involved in Isoniazid Activation (∗)

The Journal of biological chemistry, 1995-09, Vol.270 (38), p.22290-22295

1995

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Selective inhibition of bacterial dihydroorotate dehydrogenases by thiadiazolidinediones

Biochemical pharmacology, 2000-08, Vol.60 (3), p.339-342

2000

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A Pre-Steady State Analysis of Ligand Binding to Human Glucokinase: Evidence for a Preexisting Equilibrium

Biochemistry (Easton), 2007-02, Vol.46 (5), p.1423-1431

2007

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Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)‑1H‑pyrazol-1-yl)methyl)phosphonate (BMS-820132)

Journal of medicinal chemistry, 2022-03, Vol.65 (5), p.4291-4317

2022

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Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors

Journal of medicinal chemistry, 2010-08, Vol.53 (15), p.5620-5628

2010

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Novel Inhibition of Porcine Pepsin by a Substituted Piperidine

The Journal of biological chemistry, 2002-08, Vol.277 (32), p.28677-28682

2002

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Kinetic studies of the active sites functioning in the quinohemoprotein fructose dehydrogenase

FEBS letters, 1993-02, Vol.318 (1), p.23-26

1993

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Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

BMC pharmacology, 2012-04, Vol.12 (1), p.2-2, Article 2

2012

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Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)

Archives of biochemistry and biophysics, 2006, Vol.445 (1), p.9-18

2006

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P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice

The Journal of pharmacology and experimental therapeutics, 2008-08, Vol.326 (2), p.502

2008

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Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (22), p.6916-6924

2011

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Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Mechanism of Inhibition for BMS-791325, a Novel Non-nucleoside Inhibitor of Hepatitis C Virus NS5B Polymerase

Involvement of DPP‐IV catalytic residues in enzyme–saxagliptin complex formation

Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors

Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1

Parallel Synthesis of Potent, Pyrazole-Based Inhibitors of Helicobacter pylori Dihydroorotate Dehydrogenase

NADH Dehydrogenase Defects Confer Isoniazid Resistance and Conditional Lethality in Mycobacterium smegmatis

Antisense RNA to ahpC, an oxidative stress defence gene involved in isoniazid resistance, indicates that AhpC of Mycobacterium bovis has virulence properties

Evidence for Isoniazid Oxidation by Oxyferrous Mycobacterial Catalase−Peroxidase

Discovery of a novel, highly potent and orally bioavailable pyrrolidinone indole series of irreversible Myeloperoxidase (MPO) inhibitors

Helicobacter pylori-selective Antibacterials Based on Inhibition of Pyrimidine Biosynthesis

Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO)

The Role of Mn(II)-Peroxidase Activity of Mycobacterial Catalase-Peroxidase in Activation of the Antibiotic Isoniazid

Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1 H -pyrazol-1-yl)methyl)phosphonate (BMS-820132)

Purification and Characterization of the Mycobacterium smegmatis Catalase-Peroxidase Involved in Isoniazid Activation (∗)

Selective inhibition of bacterial dihydroorotate dehydrogenases by thiadiazolidinediones

A Pre-Steady State Analysis of Ligand Binding to Human Glucokinase: Evidence for a Preexisting Equilibrium

Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)‑1H‑pyrazol-1-yl)methyl)phosphonate (BMS-820132)

Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors

Novel Inhibition of Porcine Pepsin by a Substituted Piperidine

Kinetic studies of the active sites functioning in the quinohemoprotein fructose dehydrogenase

Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)

P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice

Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)

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