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Title 

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

Authors 

K LeeJ I GooH Y JungM KimS K BoovanahalliH R ParkMun-Ock KimD H KimHyun Sun LeeY Choi

Publisher 

Elsevier

Issue Date 

2012

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 22, no. 24, pp. 7456-7460

Keywords 

BenzimidazoleDGATDGAT inhibitorsObesityTriglyceridesType II diabetes

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.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2012.10.046

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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