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

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

Research output: Contribution to journalArticle

14 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)7456-7460
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number24
DOIs
Publication statusPublished - 2012 Dec 15

Keywords

  • Benzimidazole
  • DGAT
  • DGAT inhibitors
  • Obesity
  • Triglycerides
  • Type II diabetes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Lee, K., Goo, J. I., Jung, H. Y., Kim, M., Boovanahalli, S. K., Park, H. R., Kim, M. O., Kim, D. H., Lee, H. S., & Choi, Y. (2012). Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors. Bioorganic and Medicinal Chemistry Letters, 22(24), 7456-7460. https://doi.org/10.1016/j.bmcl.2012.10.046