Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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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)
  • Received : 2013.04.04
  • Accepted : 2013.05.07
  • Published : 2013.08.20
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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.

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