Synthesis and biological evaluation of aminobenzimidazole derivatives with a phenylcyclohexyl acetic acid group as anti-obesity and anti-diabetic agents |
| |
| Authors: | Hyun Jung Kwak 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 |
| |
| Institution: | 1. Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea;2. Department of Chemistry, Sogang University, Seoul 121-742, Republic of Korea;3. Department of Medicinal and Pharmaceutical Chemistry, University of Science and Technology, Daejeon 305-333, Republic of Korea |
| |
| 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 4 weeks study with DIO mouse model. |
| |
| Keywords: | Diacylglycerol acyltransferase-1 DGAT-1 Triglycerides TG Obesity Diabetes Aminobenzimidazole |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
