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

Kenichi Onda,Ryota Shiraki,Takashi Ogiyama,Kazuhiro Yokoyama,Kazuhiro Momose,Naoko Katayama,Masaya Orita,Tomohiko Yamaguchi,Masako Furutani,Noritaka Hamada,Makoto Takeuchi,Minoru Okada,Mitsuaki Ohta,Shin-ichi Tsukamoto

Bioorganic & Medicinal Chemistry（2008）

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摘要

5-Chloro-N-[(5R)-1,3,6,6-tetrafluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl]-1H-indole-2-carboxamide are potent inhibitors of human liver glycogen phosphorylase a (hLGPa) that inhibited glucagon-induced glucose output in cultured primary hepatocytes and showed oral hypoglycemic activity in diabetic db/db mice.

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关键词

Glycogen phosphorylase,Hepatic glucose output,Docking study,Hypoglycemic activity

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