2-Heteroaryl Benzimidazole Derivatives as Melanin Concentrating Hormone Receptor 1 (MCH-R1) Antagonists

Bulletin of the Korean chemical society

Chae Jo Lim¹  Kyu Yang Yi¹  Byung Ho Lee¹  Kwang-Seok Oh¹  Jeong Young Kim¹ 

关键词: Melanin concentrating hormone (MCH);    MCH-R1 antagonist;    2-Heteroaryl benzimidazole;    Obesity;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

A novel series of 2-heteroaryl substituted benzimidazole derivatives, containing the piperidinylphenyl acetamide group at the 1-position, were synthesized and evaluated as MCH-R1 antagonists. Extensive SAR investigation probing the effects of C-2 heteroaryl group led to the identification of 2-[2-(pyridin-3-yl)ethyl] analog 3o, which exhibits highly potent MCH-R1 binding activity with an IC50 value of 1 nM. This substance 3o also has low hERG binding activity, good metabolic stability, and favorable pharmacokinetic properties.

【 授权许可】

Unknown