Development of novel alkene oxindole derivatives as orally efficacious AMP-activated protein kinase activators

…, M Zhang, W Zhang, LN Zhang, T Pang…

文献索引：Yu, Li-Fang; Li, Yuan-Yuan; Su, Ming-Bo; Zhang, Mei; Zhang, Wei; Zhang, Li-Na; Pang, Tao; Zhang, Run-Tao; Liu, Bing; Li, Jing-Ya; Li, Jia; Nan, Fa-Jun ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 5 p. 475 - 480

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被引用次数: 25

摘要

Adenosine 5′-monophosphate-activated protein kinase (AMPK) is emerging as a promising drug target for its regulatory function in both glucose and lipid metabolism. Compound PT1 (5) was originally identified from high throughput screening as a small molecule activator of AMPK through the antagonization of the autoinhibition in α subunits. In order to enhance its potency at AMPK and bioavailability, structure–activity relationship ...