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Bioorg Med Chem Lett. 2013 Aug 15;23(16):4713-8. doi: 10.1016/j.bmcl.2013.05.081. Epub 2013 Jun 4.

Synthesis and biological evaluation of aminobenzimidazole derivatives with a phenylcyclohexyl acetic acid group as anti-obesity and anti-diabetic agents.

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  • 1Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea.


A series of benzimidazole derivatives with a phenylcyclohexyl acetic acid group as DGAT-1 inhibitors was developed. Among the benzimidazole series, compound 5k showed submicromolar in vitro activity toward human and mouse DGAT-1, good selectivity toward DGAT-2, human liver metabolic stability, and pharmacokinetic (PK) and safety profiles such as hERG, CYP and acute toxicity. Additionally, 5k showed good in vivo efficacy in 4weeks study with DIO mouse model.

Copyright © 2013 Elsevier Ltd. All rights reserved.


Aminobenzimidazole; DGAT-1; Diabetes; Diacylglycerol acyltransferase-1; Obesity; TG; Triglycerides

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