Synthesis and SAR investigations of novel 2-arylbenzimidazole derivatives as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists

CJ Lim, N Kim, EK Lee, BH Lee, KS Oh, S Yoo…

文献索引：Lim, Chae Jo; Kim, Nakjeong; Lee, Eun Kyoung; Lee, Byung Ho; Oh, Kwang-Seok; Yoo, Sung-Eun; Yi, Kyu Yang Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2309 - 2312

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被引用次数: 12

摘要

Compounds containing 2-arybenzimidazole ring systems linked to arylpiperidines were synthesized and evaluated as MCH-R1 antagonists. The results of structure–activity relationship studies led to the identification of compound 4c as a potent MCH-R1 antagonist (IC50= 1nM). This compound also has good metabolic stability, and favorable pharmacokinetic and brain penetration properties. However 4c was found to be potent ...