Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha sub(v) beta sub(3) integrin receptor antagonists with improved oral pharmacokinetic properties

• Published in: Bioorganic & medicinal chemistry letters Vol. 16; no. 4; pp. 845 - 849
• Main Authors: Wendt, John A, Wu, Hongwei, Stenmark, Heather G, Boys, Mark L, Downs, Victoria L, Penning, Thomas D, Chen, Barbara B, Wang, Yaping, Duffin, Tiffany, Finn, Mary Beth, Keene, Jeffery L, Engleman, VWayne, Freeman, Sandra K, Hanneke, Melanie L, Shannon, Kristen E, Nickols, Maureen A, Steininger, Christina N, Westlin, Marissa, Klover, Jon A, Westlin, William, Nickols, GAllen, Russell, Mark A
• Format: Journal Article
• Language: English
• Published: 01.02.2006
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2005.11.017

We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin alpha sub(v) beta sub(3) and show selectivity relative to the other integrins, such as alpha sub(IIb) beta sub(3) and alpha sub(v) beta sub(6). These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.