1. Synthesis of 2,5-thiazole butanoic acids as potent and selective αvβ3 integrin receptor antagonists with improved oral pharmacokinetic properties
- Author
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Mary Beth Finn, Hongwei Wu, Kristen E. Shannon, V. Wayne Engleman, Maureen A. Nickols, Jon A. Klover, Marissa Westlin, Tiffany Duffin, Christina N. Steininger, G. Allen Nickols, Thomas D. Penning, Melanie L. Hanneke, John A. Wendt, Heather Stenmark, Mark A. Russell, Jeffery L. Keene, Downs Victoria Leigh, William F. Westlin, Barbara B. Chen, Wang Yaping, Sandra K. Freeman, and Mark L. Boys
- Subjects
Integrins ,Stereochemistry ,Clinical Biochemistry ,Integrin ,Drug Evaluation, Preclinical ,Administration, Oral ,Biological Availability ,Pharmaceutical Science ,Alpha (ethology) ,Platelet Glycoprotein GPIIb-IIIa Complex ,Biochemistry ,Chemical synthesis ,Structure-Activity Relationship ,chemistry.chemical_compound ,Dogs ,Antigens, Neoplasm ,Drug Discovery ,Animals ,Structure–activity relationship ,Thiazole ,Molecular Biology ,Integrin alphaVbeta3 ,Molecular Structure ,biology ,Chemistry ,Organic Chemistry ,Haplorhini ,Rats ,Bioavailability ,Butyrates ,Thiazoles ,biology.protein ,Molecular Medicine - Abstract
We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin alpha(v)beta3 and show selectivity relative to the other integrins, such as alpha(IIb)beta3 and alpha(v)beta6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.
- Published
- 2006