Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha(v)beta3 integrin receptor antagonists with improved oral pharmacokinetic properties

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 relati...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-02, Vol.16 (4), p.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, V Wayne, Freeman, Sandra K, Hanneke, Melanie L, Shannon, Kristen E, Nickols, Maureen A, Steininger, Christina N, Westlin, Marissa, Klover, Jon A, Westlin, William, Nickols, G Allen, Russell, Mark A
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Antigens, Neoplasm
Biological Availability
Butyrates - administration & dosage
Butyrates - chemical synthesis
Butyrates - pharmacokinetics
Dogs
Drug Evaluation, Preclinical
Haplorhini
Integrin alphaVbeta3 - antagonists & inhibitors
Integrins - antagonists & inhibitors
Molecular Structure
Platelet Glycoprotein GPIIb-IIIa Complex - antagonists & inhibitors
Rats
Structure-Activity Relationship
Thiazoles - administration & dosage
Thiazoles - chemical synthesis
Thiazoles - pharmacokinetics
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Description
Summary: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.
ISSN:0960-894X
1464-3405