New thiazole derivatives as potent and selective 5-hydroxytriptamine 3 (5-HT 3) receptor agonists for the treatment of constipation

N Imanishi, K Iwaoka, H Koshio, S Nagashima…

Index: Imanishi, Naoki; Iwaoka, Kiyoshi; Koshio, Hiroyuki; Nagashima, Shin-Ya; Kazuta, Ken-Ichi; Ohta, Mitsuaki; Sakamoto, Shuichi; Ito, Hiroyuki; Akuzawa, Shinobu; Kiso, Tetsuo; Tsukamoto, Shin-Ichi; Mase, Toshiyasu Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 7 p. 1493 - 1502

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Citation Number: 16

Abstract

The syntheses and biological evaluation of a series of novel indeno [1, 2-d] thiazole derivatives are described. Several groups reported 5-HT3 receptor agonists which were mainly evaluated for their activities on the von Bezold–Jarisch reflex (B–J reflex). We discovered that tetrahydrothiazolopyridine derivative 1b had a contractile effect on the isolated guinea pig colon with weak B–J reflex. Our efforts to find a new type of 5-HT3 ...