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Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists |
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| Authors: | 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 |
| Affiliation: | Discovery R&D AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA. |
| 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). |
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