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http://dx.doi.org/10.5012/bkcs.2013.34.8.2305

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

Lim, Chae Jo (Division of Drug Discovery Research, Korea Research Institute of Chemical Technology)
Kim, Jeong Young (Division of Drug Discovery Research, Korea Research Institute of Chemical Technology)
Lee, Byung Ho (Division of Drug Discovery Research, Korea Research Institute of Chemical Technology)
Oh, Kwang-Seok (Division of Drug Discovery Research, Korea Research Institute of Chemical Technology)
Yi, Kyu Yang (Division of Drug Discovery Research, Korea Research Institute of Chemical Technology)
Publication Information
Bulletin of the Korean Chemical Society / v.34, no.8, 2013 , pp. 2305-2310 More about this Journal
Abstract
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 $IC_{50}$ value of 1 nM. This substance 3o also has low hERG binding activity, good metabolic stability, and favorable pharmacokinetic properties.
Keywords
Melanin concentrating hormone (MCH); MCH-R1 antagonist; 2-Heteroaryl benzimidazole; Obesity;
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