Bruce M. Bechle

Pfizer (United States) — United States

Chemistry · Physical Sciences

17h-index729citations27works59.02yr avg
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Research Topics

Asymmetric Synthesis and Catalysis(5), Chemical Synthesis and Analysis(5), Synthesis and Catalytic Reactions(5), Synthesis and biological activity(3), Receptor Mechanisms and Signaling(3)

Publications27 total

A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19
Journal of Medicinal Chemistry·2024· 59 citedOpen Access
Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels
Nature Communications·2023· 27 citedOpen Access
Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain
Journal of Medicinal Chemistry·2018· 35 citedOpen Access
Development of a scalable synthetic route towards a 2,2,6-trisubstituted chiral morpholine via stereoselective hydroalkoxylation
Tetrahedron Letters·2018· 6 cited
Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes
Bioorganic & Medicinal Chemistry Letters·2017· 27 citedOpen Access
Discovery of Clinical Candidate 4-[2-(5-Amino-1<i>H</i>-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-<i>N</i>-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na<sub>V</sub>1.7
Journal of Medicinal Chemistry·2017· 83 citedOpen Access
One-Pot Synthesis of α-Branched <i>N</i>-Acylamines via Titanium-Mediated Condensation of Amides, Aldehydes, and Organometallics
Organic Letters·2017· 9 cited
ChemInform Abstract: Diastereoselective Synthesis of β‐Heteroaryl syn‐α‐Methyl‐β‐amino Acid Derivatives via a Double Chiral Auxiliary Approach.
ChemInform·2013
PF-04859989 as a template for structure-based drug design: Identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency
Bioorganic & Medicinal Chemistry Letters·2013· 31 citedOpen Access
Diastereoselective Synthesis of β-Heteroaryl <i>syn</i>-α-Methyl-β-Amino Acid Derivatives via a Double Chiral Auxiliary Approach
Organic Letters·2013· 12 cited
Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions
ACS Medicinal Chemistry Letters·2012· 23 citedOpen Access
Discovery of hydroxamate bioisosteres as KAT II inhibitors with improved oral bioavailability and pharmacokinetics
MedChemComm·2012· 20 cited
Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia
ACS Medicinal Chemistry Letters·2012· 88 citedOpen Access
Synthesis of ortho-substituted nitroaromatics via improved Negishi coupling conditions
Tetrahedron Letters·2011· 15 cited
A General Strategy for the Synthesis of Cyclic <i>N</i>-Aryl Hydroxamic Acids via Partial Nitro Group Reduction
The Journal of Organic Chemistry·2011· 21 cited
Discovery Tactics To Mitigate Toxicity Risks Due to Reactive Metabolite Formation with 2-(2-Hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-<i>d</i>]pyrimidin-4(3<i>H</i>)-one Derivatives, Potent Calcium-Sensing Receptor Antagonists and Clinical Candidate(s) for the Treatment of Osteoporosis
Chemical Research in Toxicology·2010· 25 cited
Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists
Bioorganic & Medicinal Chemistry Letters·2009· 25 cited
Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists
Bioorganic & Medicinal Chemistry Letters·2009· 51 citedOpen Access
Chemically-enabled synthesis of 1,2,3,4-tetrahydroisoquinolin-1-ones
Tetrahedron Letters·2009· 8 cited
ChemInform Abstract: Selective Inhibition of the Tyrosine Kinase pp60c‐src by Analogues of 5,10‐Dihydropyrimido(4,5‐b)quinolin‐4(1H)‐one.
ChemInform·1995
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Frequent Co-authors

Robert L. Dow(8), Jamison B. Tuttle(7), Patrick R. Verhoest(7), Amy B. Dounay(6), Edelweiss Evrard(6), Matthew S. Corbett(6), Joseph S. Warmus(6), Xinmin Gan(5), Somraj Ghosh(5), Laura A. McAllister(5), Vinod D. Parikh(5), Thomas T. Chou(5), David C. Blakemore(5), Jianmin Sun(5), Jayvardhan Pandit(4), Michelle A. Salafia(4), Laura E. Zawadzke(4), Amit S. Kalgutkar(4), Kenneth J. DiRico(4), Robert M. Oliver(4)