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 | |
| Publication status | Published - 2012 Dec 15 |
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Keywords
- Benzimidazole
- DGAT
- DGAT inhibitors
- Obesity
- Triglycerides
- Type II diabetes
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery
- Organic Chemistry
- Molecular Medicine
- Molecular Biology
- Clinical Biochemistry
- Biochemistry
Cite this
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
}
TY - JOUR
T1 - Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors
AU - Lee, Kyeong
AU - Goo, Ja Il
AU - Jung, Hwa Young
AU - Kim, Minkyoung
AU - Boovanahalli, Shanthaveerappa K.
AU - Park, Hye Ran
AU - Kim, Mun Ock
AU - Kim, Dong Hyun
AU - Lee, Hyun Sun
AU - Choi, Yongseok
PY - 2012/12/15
Y1 - 2012/12/15
N2 - 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.
AB - 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.
KW - Benzimidazole
KW - DGAT
KW - DGAT inhibitors
KW - Obesity
KW - Triglycerides
KW - Type II diabetes
UR - http://www.scopus.com/inward/record.url?scp=84870252419&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84870252419&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2012.10.046
DO - 10.1016/j.bmcl.2012.10.046
M3 - Article
C2 - 23141914
AN - SCOPUS:84870252419
VL - 22
SP - 7456
EP - 7460
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 24
ER -