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

doi:10.1016/j.bmcl.2012.10.046

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

Department of Biotechnology

Research output: Contribution to journal › Article › peer-review

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 language	English
Pages (from-to)	7456-7460
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	22
Issue number	24
DOIs	https://doi.org/10.1016/j.bmcl.2012.10.046
Publication status	Published - 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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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.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 22, No. 24, 15.12.2012, p. 7456-7460.

Research output: Contribution to journal › Article › peer-review

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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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