Synthesis and structure–activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT 2B and 5-HT 7 receptor antagonists

A Moritomo, H Yamada, T Watanabe, H Itahana…

Index: Moritomo, Ayako; Yamada, Hiroyoshi; Watanabe, Toshihiro; Itahana, Hirotsune; Akuzawa, Shinobu; Okada, Minoru; Ohta, Mitsuaki Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 24 p. 7841 - 7852

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Citation Number: 8

Abstract

Abstract To identify potent dual 5-HT 2B and 5-HT 7 receptor antagonists, we synthesized a series of novel carbonyl guanidine derivatives and examined their structure–activity relationships. Among these compounds, N-(9-hydroxy-9H-fluorene-2-carbonyl) guanidine (10) had a good in vitro profile, that is, potent affinity for human 5-HT 2B and 5-HT 7 receptor subtypes (K i= 1.8 nM and K i= 17.6 nM, respectively) and high selectivity over 5-HT 2A, 5- ...