Yang Z.,Discovery R and D AMRI |
Fairfax D.J.,Discovery R and D AMRI |
Maeng J.-H.,Discovery R and D AMRI |
Masih L.,Discovery R and D AMRI |
And 23 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010
A new class of 2-substituted benzoxazole carboxamides are presented as potent functional 5-HT3 receptor antagonists. The chemical series possesses nanomolar in vitro activity against human 5-HT3A receptors. A chemistry optimization program was conducted and identified 2-aminobenzoxazoles as orally active 5-HT3 receptor antagonists with good metabolic stability. These novel analogues possess drug-like characteristics and have potential utility for the treatment of diseases attributable to improper 5-HT3 receptor function, especially diarrhea predominant irritable bowel syndrome (IBS-D). © 2010 Elsevier Ltd. All rights reserved.