Synthesis and structure–activity relationships of a series of substituted 2-(1H-furo [2, 3-g] indazol-1-yl) ethylamine derivatives as 5-HT 2C receptor agonists

…, Y Kimura, K Hatanaka, Y Naitou, F Wanibuchi…

Index: Shimada, Itsuro; Maeno, Kyoichi; Kazuta, Ken-ichi; Kubota, Hideki; Kimizuka, Tetsuya; Kimura, Yasuharu; Hatanaka, Ken-ichi; Naitou, Yuki; Wanibuchi, Fumikazu; Sakamoto, Shuichi; Tsukamoto, Shin-ichi Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 4 p. 1966 - 1982

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Citation Number: 30

Abstract

A series of novel indazole derivatives were synthesized, and their structure–activity relationships examined in order to identify potent and selective 5-HT2C receptor agonists. Among these compounds,(S)-2-(7-ethyl-1H-furo [2, 3-g] indazol-1-yl)-1-methylethylamine (YM348) had a good in vitro profile, that is, high agonistic activity to the human 5-HT2C receptor subtype (EC50= 1.0 nM) and high selectivity over 5-HT2A receptors. This ...