GSBS Student Publications

Title

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor

UMMS Affiliation

Graduate School of Biomedical Sciences; Bristol-Myers Squibb

Date

3-4-2008

Document Type

Article

Medical Subject Headings

Animals; Arthritis; Caco-2 Cells; Cell Membrane Permeability; Cells, Cultured; Crystallography, X-Ray; Cytochrome P-450 Enzyme System; Ether-A-Go-Go Potassium Channels; Humans; Lipopolysaccharides; Male; Mice; Microsomes, Liver; Mitogen-Activated Protein Kinase 14; Molecular Structure; Monocytes; Protein Kinase Inhibitors; synthesis; Rats; Rats, Inbred Lew; Structure-Activity Relationship; Thiazoles; Tumor Necrosis Factor-alpha

Disciplines

Life Sciences | Medicine and Health Sciences

Abstract

A novel structural class of p38alpha MAP kinase inhibitors has been identified via iterative SAR studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38alpha inhibitor that is orally efficacious in rodent models of acute and chronic inflammation.

Rights and Permissions

Citation: Bioorg Med Chem Lett. 2008 Mar 15;18(6):1762-7. Epub 2008 Feb 16. Link to article on publisher's site

DOI of Published Version

10.1016/j.bmcl.2008.02.031

Related Resources

Link to Article in PubMed

Journal Title

Bioorganic and medicinal chemistry letters

PubMed ID

18313298