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

Lee, Kyeong; Goo, Ja-Il; Jung, Hwa Young; Kim, Minkyoung; Boovanahalli, Shanthaveerappa K.; Park, Hye Ran; Kim, Mun-Ock; Kim, Dong-Hyun; Lee, Hyun Sun; Choi, Yongseok

doi:10.1016/j.bmcl.2012.10.046

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

Lee, Kyeong;
Goo, Ja-Il;
Jung, Hwa Young;
Kim, Minkyoung;
Boovanahalli, Shanthaveerappa K.;
... Choi, Yongseok;
외 4명

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초록

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 mu M) 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. (C) 2012 Elsevier Ltd. All rights reserved.

키워드

Obesity; Type II diabetes; Triglycerides; DGAT; DGAT inhibitors; Benzimidazole; OBESITY; POTENT

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

저자: Lee, Kyeong; Goo, Ja-Il; Jung, Hwa Young; Kim, Minkyoung; Boovanahalli, Shanthaveerappa K.; Park, Hye Ran; Kim, Mun-Ock; Kim, Dong-Hyun; Lee, Hyun Sun; Choi, Yongseok

DOI: 10.1016/j.bmcl.2012.10.046

발행일: 2012-12-15

유형: Article

저널명: Bioorganic & Medicinal Chemistry Letters

권: 22

호: 24

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