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Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors
- Authors
- 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
- Issue Date
- 15-12월-2012
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Obesity; Type II diabetes; Triglycerides; DGAT; DGAT inhibitors; Benzimidazole
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.22, no.24, pp.7456 - 7460
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 22
- Number
- 24
- Start Page
- 7456
- End Page
- 7460
- ISSN
- 0960-894X
- 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 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.
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Collections - Graduate School > Department of Biotechnology > 1. Journal Articles
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