MGAT2 inhibitor decreases liver fibrosis and inflammation in murine NASH models and reduces body weight in human adults with obesity

…, LM Kopcho, R Ammar, J Smith, P Devasthale… - Cell Metabolism, 2022 - cell.com
… , CDAHFD vehicle, 0.3 mg/kg, and 3.0 mg/kg BMS-963272 groups, respectively (p < 0.001
and p < 0.01 for control diet and 3.0 mg/kg BMS-963272 versus CDAHFD vehicle). Plasma …

Design and Synthesis of N-[(4-Methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a Novel …

PV Devasthale, S Chen, Y Jeon, F Qu… - Journal of Medicinal …, 2005 - ACS Publications
Muraglitazar/BMS-298585 (2) has been identified as a non-thiazolidinedione PPAR α/γ dual
agonist that shows potent activity in vitro at human PPARα (EC 50 = 320 nM) and PPARγ (…

Muraglitazar, a novel dual (α/γ) peroxisome proliferator–activated receptor activator, improves diabetes and other metabolic abnormalities and preserves β-cell …

…, H Zhang, W Fenderson, S Chen, P Devasthale… - Diabetes, 2006 - Am Diabetes Assoc
… The gels were blotted to nylon membranes and hybridized to 32 P-cDNA probes according
to standard procedures. The radioactivity in the hybridized bands was counted on an Instant …

Monoacylglycerol Acyltransferase 2 (MGAT2) Inhibitors for the Treatment of Metabolic Diseases and Nonalcoholic Steatohepatitis (NASH) Miniperspective

P Devasthale, D Cheng - Journal of Medicinal Chemistry, 2018 - ACS Publications
… The authors declare the following competing financial interest(s): Pratik Devasthale and Dong
… Pratik Devasthale received his Ph. D. from the University of Kansas under the guidance of …

Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2, 4 …

P Devasthale, Y Wang, W Wang, J Fevig… - Journal of Medicinal …, 2013 - ACS Publications
Optimization of a 5-oxopyrrolopyridine series based upon structure–activity relationships (SARs)
developed from our previous efforts on a number of related bicyclic series yielded …

Design, synthesis and structure–activity relationships of azole acids as novel, potent dual PPAR α/γ agonists

H Zhang, DE Ryono, P Devasthale, W Wang… - Bioorganic & Medicinal …, 2009 - Elsevier
The design, synthesis and structure–activity relationships of a novel series of N-phenyl-substituted
pyrrole, 1,2-pyrazole and 1,2,3-triazole acid analogs as PPAR ligands are outlined. …

Screening hit to clinical candidate: discovery of BMS-963272, a potent, selective MGAT2 inhibitor for the treatment of metabolic disorders

…, D Cheng, RM Lawrence, P Devasthale - Journal of Medicinal …, 2021 - ACS Publications
MGAT2 inhibition is a potential therapeutic approach for the treatment of metabolic disorders.
High-throughput screening of the BMS internal compound collection identified the aryl …

Identification of a nonbasic melanin hormone receptor 1 antagonist as an antiobesity clinical candidate

WN Washburn, M Manfredi, P Devasthale… - Journal of medicinal …, 2014 - ACS Publications
Identification of MCHR1 antagonists with a preclinical safety profile to support clinical
evaluation as antiobesity agents has been a challenge. Our finding that a basic moiety is not …

Discovery of azetidinone acids as conformationally-constrained dual PPARα/γ agonists

W Wang, P Devasthale, D Farrelly, L Gu… - Bioorganic & medicinal …, 2008 - Elsevier
A novel class of azetidinone acid-derived dual PPARα/γ agonists has been synthesized for
the treatment of diabetes and dyslipidemia. The preferred stereochemistry in this series for …

Generation of functional diversity via nitroaldol condensations of α-aminoacid aldehydes—A new and stereocontrolled route to acyclic 1, 3-diamino-2-alcohols

S Hanessian, PV Devasthale - Tetrahedron letters, 1996 - Elsevier
Condensations of N,N-dibenzyl α-amino aldehydes with nitroalkanes mediated by
tetrabutylammonium fluoride proceed in excellent yields and selectivites. This affords rapid and …