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Synthesis and SAR investigations of novel 2-arylbenzimidazole derivatives as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists |
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| Authors: | Lim Chae Jo Kim Nakjeong Lee Eun Kyoung Lee Byung Ho Oh Kwang-Seok Yoo Sung-eun Yi Kyu Yang |
| Affiliation: | a Bio-organic Science Division, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon 305-600, Republic of Korea b Department of Medicinal and Pharmaceutical Chemistry, University of Science and Technology, Yuseong-gu, Daejeon 305-350, Republic of Korea |
| Abstract: | 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 = 1 nM). This compound also has good metabolic stability, and favorable pharmacokinetic and brain penetration properties. However 4c was found to be potent inhibitor of the hERG potassium channel. |
| Keywords: | Melanin-concentrating hormone (MCH) MCH-R1 antagonists 2-Arylbenzimidazole Obesity |
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