Synthesis of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives as inhibitors of human liver glycogen phosphorylase a

…, Y Yonetoku, K Negoro, K Momose, N Katayama…

文献索引：Onda, Kenichi; Suzuki, Takayuki; Shiraki, Ryota; Yonetoku, Yasuhiro; Negoro, Kenji; Momose, Kazuhiro; Katayama, Naoko; Orita, Masaya; Yamaguchi, Tomohiko; Ohta, Mitsuaki; Tsukamoto, Shin-ichi Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 10 p. 5452 - 5464

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被引用次数: 18

摘要

A series of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives were prepared and evaluated as inhibitors of human liver glycogen phosphorylase a (hLGPa). One compound, 5-chloro-N-[4-(1, 2-dihydroxyethyl) phenyl]-1H-indole-2-carboxamide (2f), inhibited hLGPa with an IC50 of 0.90 μM. The pyridine analogue of 2f showed inhibitory activity of glucagon- induced glucose output in cultured primary hepatocytes with an IC50 of 0.62 μM and oral ...