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

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

Hyun Jung Kwak ¹, Yu Mi Pyun, Ji Young Kim, Haushabhau S Pagire, Ki Young Kim, Kwang Rok Kim, Sang Dal Rhee, Won Hoon Jung, Jin Sook Song, Myung Ae Bae, Duck Hyung Lee, Jin Hee Ahn

Affiliations

Affiliation

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

PMID: 23810496 DOI: 10.1016/j.bmcl.2013.05.081

Abstract

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.

Keywords

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

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