Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists

…, N Takenaga, A Ishihara, S Tokita, A Kanatani…

Index: Haga, Yuji; Mizutani, Sayaka; Naya, Akira; Kishino, Hiroyuki; Iwaasa, Hisashi; Ito, Masahiko; Ito, Junko; Moriya, Minoru; Sato, Nagaaki; Takenaga, Norihiro; Ishihara, Akane; Tokita, Shigeru; Kanatani, Akio; Ohtake, Norikazu Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 2 p. 883 - 893

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Citation Number: 6

Abstract

The design, synthesis and structure–activity relationships of a novel class of N- phenylpyridone MCH1R antagonists are described. The core part of the N-phenylpyridone structure was newly designed and the side chain moieties that were attached to the core part were extensively explored. As a result of optimization of the N-phenylpyridone leads, we successfully developed the orally available, and brain-penetrable MCH1R selective ...