Synthesis and SAR study of pyrrolo [3, 4-b] pyridin-7 (6H)-one derivatives as melanin concentrating hormone receptor 1 (MCH-R1) antagonists

CJ Lim, JY Kim, BH Lee, KS Oh, KY Yi

文献索引：Lim, Chae Jo; Kim, Ji Young; Lee, Byung Ho; Oh, Kwang-Seok; Yi, Kyu Yang Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 6 p. 1736 - 1739

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被引用次数: 6

摘要

The discovery and optimization of novel pyrrolo [3, 4-b] pyridin-7 (6H)-one MCH-R1 antagonists are described. A systematic SAR study probing the effects of aryl-, benzyl-and arylthio-substituents at the 2-position of the pyrrolo [3, 4-b] pyridin-7 (6H)-ones led to identification of the 2-[(4-fluorophenyl) thio] derivative 7b as a highly potent MCH-R1 antagonist. This compound also has favorable pharmacokinetic properties along with a ...