1081111-23-0Relevant articles and documents
Synthesis and SAR investigations of novel 2-arylbenzimidazole derivatives as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists
Lim, Chae Jo,Kim, Nakjeong,Lee, Eun Kyoung,Lee, Byung Ho,Oh, Kwang-Seok,Yoo, Sung-Eun,Yi, Kyu Yang
, p. 2309 - 2312 (2011/05/15)
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.