| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372319 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
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,