Design, synthesis, and pharmacological evaluation of N-bicyclo-5-chloro-1H-indole-2-carboxamide derivatives as potent glycogen phosphorylase inhibitors

…, R Shiraki, T Ogiyama, K Yokoyama, K Momose…

Index: Onda, Kenichi; Shiraki, Ryota; Ogiyama, Takashi; Yokoyama, Kazuhiro; Momose, Kazuhiro; Katayama, Naoko; Orita, Masaya; Yamaguchi, Tomohiko; Furutani, Masako; Hamada, Noritaka; Takeuchi, Makoto; Okada, Minoru; Ohta, Mitsuaki; Tsukamoto, Shin-ichi Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 23 p. 10001 - 10012

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Citation Number: 8

Abstract

As a result of the various N-bicyclo-5-chloro-1H-indole-2-carboxamide derivatives with a hydroxy moiety synthesized in an effort to discover novel glycogen phosphorylase (GP) inhibitors, 5-chloro-N-(5-hydroxy-5, 6, 7, 8-tetrahydronaphthalen-2-yl)-1H-indole-2- carboxamide (5b) was found to have potent inhibitory activity. The introduction of fluorine atoms both at a position adjacent to the hydroxy group and in the central benzene moiety ...