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Brief Article

Orally Active Benzoxazole Derivative as 5-HT₃ Receptor Partial Agonist for Treatment of Diarrhea-Predominant Irritable Bowel Syndrome

Supporting Info

Satoshi Yoshida,* Sojiro Shiokawa, Ken-ichi Kawano, Tomoko Ito, Hiroshi Murakami, Hisashi Suzuki, and Yasuo Sato

Pharmaceutical Research Department Meiji Seika Kaisha, Ltd., 760 Morooka-Cho, Kohoku-ku, Yokohama 222-8567 Japan

J. Med. Chem., 2005, 48 (22), pp 7075–7079

DOI: 10.1021/jm050209t

Publication Date (Web): October 12, 2005

To whom correspondence should be addressed. Tel: +81-45-545-3133. Fax: +81-45-541-0667. E-mail: satoshi_yoshida@meiji.co.jp.

Abstract

During our search for therapeutic agents to treat diarrhea-predominant IBS, we found that 2-substituted benzoxazole derivatives have a characteristic 5-HT₃ receptor partial agonist activity with high affinity. Some of these compounds showed high in vitro metabolical stability, and 6g showed marked antidiarrhetic activity with little side effect of constipation in in vivo tests. Our results indicate that 5-HT₃ receptor partial agonists might be superior as therapeutic agents to the drugs currently used for IBS treatment.

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Published In Issue November 03, 2005
Received March 8, 2005

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Brief Article

Orally Active Benzoxazole Derivative as 5-HT₃ Receptor Partial Agonist for Treatment of Diarrhea-Predominant Irritable Bowel Syndrome