Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors

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Title
Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors
Author(s)
K Lee; J I Goo; H Y Jung; M Kim; S K Boovanahalli; H R Park; Mun-Ock Kim; D H Kim; Hyun Sun Lee; Y Choi
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 22, no. 24, pp. 7456-7460
Publication Year
2012
Abstract
A novel series of benzimidazole derivatives was prepared and evaluated for their diacylglycerol acyltransferase (DGAT) inhibitory activity using microsome from rat liver. Among the newly synthesized compounds, furfurylamine containing benzimidazole carboxamide 10j showed the most potent DGAT inhibitory effect (IC50= 4.4 μM) and inhibited triglyceride formation in HepG2 cells. Furthermore, compound 10j reduced body weight gain of Institute of Cancer Research mice on a high-fat diet and decreased levels of total triglyceride, total cholesterol, and LDL-cholesterol in the blood accompanied with a significant increase in HDL-cholesterol level.
Keyword
BenzimidazoleDGATDGAT inhibitorsObesityTriglyceridesType II diabetes
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2012.10.046
Type
Article
Appears in Collections:
Ochang Branch Institute > Natural Product Research Center > 1. Journal Articles
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