Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors |
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| Authors: | Kyeong Lee 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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| Institution: | 1. College of Pharmacy, Dongguk University-Seoul, Seoul 100-715, Republic of Korea;2. College of Life Sciences and Biotechnology, Korea University, Seoul 136-701, Republic of Korea;3. Chemical Biology Research Center, KRIBB, Ochang, Cheongwon, Chungbuk 363-883, Republic of Korea;4. College of Pharmacy, Kyung Hee University, Seoul 130-701, Republic of Korea |
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| 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. |
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