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. 2012 Dec 15;22(24):7456-60.
doi: 10.1016/j.bmcl.2012.10.046. Epub 2012 Oct 17.

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

Kyeong Lee  1 , Ja-Il Goo, Hwa Young Jung, Minkyoung Kim, Shanthaveerappa K Boovanahalli, Hye Ran Park, Mun-Ock Kim, Dong-Hyun Kim, Hyun Sun Lee, Yongseok Choi
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Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors

Kyeong Lee et al. Bioorg Med Chem Lett. .

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 (IC(50)=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.

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