Literature DB >> 16250667

Orally active benzoxazole derivative as 5-HT3 receptor partial agonist for treatment of diarrhea-predominant irritable bowel syndrome.

Satoshi Yoshida1, Sojiro Shiokawa, Ken-ichi Kawano, Tomoko Ito, Hiroshi Murakami, Hisashi Suzuki, Yasuo Sato.   

Abstract

During our search for therapeutic agents to treat diarrhea-predominant IBS, we found that 2-substituted benzoxazole derivatives have a characteristic 5-HT(3) 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-HT(3) receptor partial agonists might be superior as therapeutic agents to the drugs currently used for IBS treatment.

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Year:  2005        PMID： 16250667     DOI： 10.1021/jm050209t

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  5 in total

1.  VUF10166, a novel compound with differing activities at 5-HT₃A and 5-HT₃AB receptors.

Authors:  A J Thompson; M H P Verheij; I J P de Esch; S C R Lummis
Journal:  J Pharmacol Exp Ther       Date:  2012-02-03       Impact factor: 4.030

2.  First cascade Mitsunobu reactions for the synthesis of 2-benzoxazole-N-phenyl and 2-benzimidazole-N-phenyl derivatives.

Authors:  Yu Yan; Qifei Zhong; Nan Zhao; Gang Liu
Journal:  Mol Divers       Date:  2011-11-30       Impact factor: 2.943

3.  Two novel α7 nicotinic acetylcholine receptor ligands: in vitro properties and their efficacy in collagen-induced arthritis in mice.

Authors:  Marjolein A van Maanen; Roger L Papke; Frieda A Koopman; Jessica Koepke; Lisette Bevaart; Roger Clark; Diana Lamppu; Daniel Elbaum; Gregory J LaRosa; Paul P Tak; Margriet J Vervoordeldonk
Journal:  PLoS One       Date:  2015-01-24       Impact factor: 3.240

4.  The Synthesis of 2-Aminobenzoxazoles Using Reusable Ionic Liquid as a Green Catalyst under Mild Conditions.

Authors:  Ya Zhou; Zhiqing Liu; Tingting Yuan; Jianbin Huang; Chenjiang Liu
Journal:  Molecules       Date:  2017-04-02       Impact factor: 4.411

5.  5-Fluorotryptamine is a partial agonist at 5-HT3 receptors, and reveals that size and electronegativity at the 5 position of tryptamine are critical for efficient receptor function.

Authors:  Kiowa S Bower; Kerry L Price; Laura E C Sturdee; Mariza Dayrell; Dennis A Dougherty; Sarah C R Lummis
Journal:  Eur J Pharmacol       Date:  2007-11-17       Impact factor: 4.432
  5 in total

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