Cited 19 time in
- Title
- Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors
- Author(s)
- K Lee; J I Goo; H Y Jung; M Kim; S K Boovanahalli; H R Park; Mun-Ock Kim; D H Kim; Hyun Sun Lee; Y Choi
- Bibliographic Citation
- Bioorganic & Medicinal Chemistry Letters, vol. 22, no. 24, pp. 7456-7460
- Publication Year
- 2012
- 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.
- Keyword
- BenzimidazoleDGATDGAT inhibitorsObesityTriglyceridesType II diabetes
- ISSN
- 0960-894X
- Publisher
- Elsevier
- DOI
- http://dx.doi.org/10.1016/j.bmcl.2012.10.046
- Type
- Article
- Appears in Collections:
- Ochang Branch Institute > Natural Product Research Center > 1. Journal Articles
- Files in This Item:
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