906095-11-2Relevant academic research and scientific papers
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists
Yang, Zhicai,Fairfax, David J.,Maeng, Jun-Ho,Masih, Liaqat,Usyatinsky, Alexander,Hassler, Carla,Isaacson, Soshanna,Fitzpatrick, Kevin,Deorazio, Russell J.,Chen, Jianqing,Harding, James P.,Isherwood, Matthew,Dobritsa, Svetlana,Christensen, Kevin L.,Wierschke, Jonathan D.,Bliss, Brian I.,Peterson, Lisa H.,Beer, Cathy M.,Cioffi, Christopher,Lynch, Michael,Rennells, W. Martin,Richards, Justin J.,Rust, Timothy,Khmelnitsky, Yuri L.,Cohen, Marlene L.,Manning, David D.
scheme or table, p. 6538 - 6541 (2010/11/21)
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).
Benzoxazole carboxamides for treating CINV and IBS-D
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Page/Page column 11, (2008/06/13)
Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds that exhibit central activity are useful in treating CINV; those that inhibit peripheral receptors are useful to treat IBS-D.
