Hybrids of coumarin-indole: design, synthesis and biological evaluation in Triton WR-1339 and high-fat diet induced hyperlipidemic rat modelsThe authors declare no competing interests.Electronic supplementary information (ESI) available: 1H NMR, 13C NMR, LC-MS/MS, Biological details. See DOI: 10.1039/c6md00283h
In this study, a series of coumarin-indole hybrids have been synthesized and evaluated for their lipid lowering activity. Preliminary biological screening of the synthesized compounds was undertaken in an in vitro model of the HMG-CoA reductase enzyme, and the activity was confirmed in Triton WR-133...
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Main Authors | , , , , , , , , , , , , , |
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Format | Journal Article |
Published |
14.09.2016
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Online Access | Get full text |
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Summary: | In this study, a series of coumarin-indole hybrids have been synthesized and evaluated for their lipid lowering activity. Preliminary biological screening of the synthesized compounds was undertaken in an
in vitro
model of the HMG-CoA reductase enzyme, and the activity was confirmed in Triton WR-1339 induced hyperlipidemic rats. Among the hybrids, compound
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was found to be the best as it significantly reduced the serum and hepatic lipid profiles in an HFD-fed hyperlipidemic rat model. The mechanism of action seems to be associated with the regulation of HMG-CoA reductase activity in the liver, which is in good agreement with binding mode studies. Compound
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exhibited favorable pharmacokinetic behavior for its oral administration, which underscores the potential of this template as a new class of hypolipidemic agents.
Lipid lowering activity of novel coumarin-indole hybrids has been demonstrated. |
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Bibliography: | 1 13 The authors declare no competing interests. C NMR, LC-MS/MS, Biological details. See DOI Electronic supplementary information (ESI) available H NMR 10.1039/c6md00283h |
ISSN: | 2040-2503 2040-2511 |
DOI: | 10.1039/c6md00283h |