Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.

Wu Du,James P Jewell,Linus S Lin,Vincent J Colandrea,Jing Chen Xiao,Julie Lao,Chun-Pyn Shen,Thomas J Bateman,Vijay Bhasker G Reddy,Sookhee N Ha,Shrenik K Shah,Tung M Fong,Jeffrey J Hale,William K Hagmann

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

A series of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamides were prepared by a divergent synthesis. Their potential as CB1R inverse agonists, metabolism and binding mode were studied.

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关键词

CB1R,Inverse agonist,Obesity,Synthesis,Metabolism

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