Synthesis of a novel series of benzocycloalkene derivatives as melatonin receptor agonists

…, T Yamano, M Yamashita, K Kato, K Hirai…

Index: Fukatsu, Kohji; Uchikawa, Osamu; Kawada, Mitsuru; Yamano, Toru; Yamashita, Masayuki; Kato, Koki; Hirai, Keisuke; Hinuma, Shuji; Miyamoto, Masaomi; Ohkawa, Shigenori Journal of Medicinal Chemistry, 2002 , vol. 45, # 19 p. 4212 - 4221

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Citation Number: 47

Abstract

We synthesized a novel series of benzocycloalkene derivatives and evaluated their binding affinities to melatonin receptors. To control the spatial position of the amide group, one of the important pharmacophores, we incorporated an endo double bond, an exo double bond (E- and Z-configurations), and a chiral center (R-and S-configurations) at position 1. The indan derivatives with the S-configuration at position 1 were the most promising in terms of ...