| Literature DB >> 20889341 |
Zhicai Yang1, David J Fairfax, Jun-Ho Maeng, Liaqat Masih, Alexander Usyatinsky, Carla Hassler, Soshanna Isaacson, Kevin Fitzpatrick, Russell J DeOrazio, Jianqing Chen, James P Harding, Matthew Isherwood, Svetlana Dobritsa, Kevin L Christensen, Jonathan D Wierschke, Brian I Bliss, Lisa H Peterson, Cathy M Beer, Christopher Cioffi, Michael Lynch, W Martin Rennells, Justin J Richards, Timothy Rust, Yuri L Khmelnitsky, Marlene L Cohen, David D Manning.
Abstract
A new class of 2-substituted benzoxazole carboxamides are presented as potent functional 5-HT(3) receptor antagonists. The chemical series possesses nanomolar in vitro activity against human 5-HT(3)A receptors. A chemistry optimization program was conducted and identified 2-aminobenzoxazoles as orally active 5-HT(3) 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-HT(3) receptor function, especially diarrhea predominant irritable bowel syndrome (IBS-D).Entities:
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Year: 2010 PMID： 20889341 DOI： 10.1016/j.bmcl.2010.09.038
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823