Melanin-concentrating hormone receptor 1 antagonists: Synthesis, structure–activity relationship, docking studies, and biological evaluation of 2, 3, 4, 5-tetrahydro-1H- …

S Kasai, M Kamaura, M Kamata, K Aso, H Ogino…

Index: Kasai, Shizuo; Kamaura, Masahiro; Kamata, Makoto; Aso, Kazuyoshi; Ogino, Hitomi; Nakano, Yoshihide; Watanabe, Kaoru; Kaisho, Tomoko; Tawada, Michiko; Nagisa, Yasutaka; Takekawa, Shiro; Kato, Koki; Suzuki, Nobuhiro; Ishihara, Yuji Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 21 p. 6261 - 6273

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Citation Number: 6

Abstract

Melanin-concentrating hormone receptor 1 (MCHR1) antagonists have been studied as potential agents for the treatment of obesity. Initial structure–activity relationship studies of in- house hit compound 1a and subsequent optimization studies resulted in the identification of tetrahydroisoquinoline derivative 23, 1-(2-acetyl-1, 2, 3, 4-tetrahydroisoquinolin-7-yl)-4-[4-(4- chlorophenyl) piperidin-1-yl] butan-1-one, as a potent hMCHR1 antagonist. A homology ...