• Bulletin of the Korean Chemical Society
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• v.33 no.7
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• pp.2389-2392
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• 2012

• Bulletin of the Korean Chemical Society
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• v.34 no.8
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• pp.2305-2310
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• 2013

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.

• Bulletin of the Korean Chemical Society
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• v.34 no.12
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• pp.3851-3854
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• 2013