Synthesis, characterization, molecular modelling and biological evaluation of substituted benzo (h) chromene-3-carboxylate derivatives as a potential agent for the treatment of hyperlipidemia
By: Verma, V. S
.
Contributor(s): Badwaik, H. R.
Publisher: Mumbai Indian Journal of Pharmaceutical Science 2022Edition: Vol.84(2), Mar-Apr.Description: 453-464p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
Indian journal of pharmaceutical sciencesSummary: Hyperlipidemia is characterized by a rise in high-density lipoproteins and decreases in low-density
lipoproteins and triglyceride level in blood serum. Numerous prescription drugs for hyperlipidemia are
available, but each has significant side effects. Many works were motivated in this area by the significant
pharmacological action of fused chromene. Throughout the present research, new substituted derivatives
were synthesized and tested for the anti-hyperlipidemic activity for benzo[h]chromene-3 carboxylate
derivatives. Molecules docking showed that compound Vf has greater energy affinity binding values
(-12.898 kcal/mol) with 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase enzyme compared with
atorvastatin (-11.8605 kcal/mol). All synthesized compounds (Va-l) were able to decreases total cholesterol,
low-density lipoproteins and triglycerides and increased high-density lipoproteins and very low-density
lipoprotein in hyperlipidemic rats. Compounds Va-l have a good affinity towards 3-hydroxy-3-methyl-
glutaryl-coenzyme A reductase enzyme. High yield, good affinity, a nontoxic and low cardiac risk with
potential antihyperlipidemic activity make these compounds the possible lead for future research.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|
Articles Abstract Database
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School of Pharmacy Archieval Section | Not for loan | 2022-2187 |
Hyperlipidemia is characterized by a rise in high-density lipoproteins and decreases in low-density
lipoproteins and triglyceride level in blood serum. Numerous prescription drugs for hyperlipidemia are
available, but each has significant side effects. Many works were motivated in this area by the significant
pharmacological action of fused chromene. Throughout the present research, new substituted derivatives
were synthesized and tested for the anti-hyperlipidemic activity for benzo[h]chromene-3 carboxylate
derivatives. Molecules docking showed that compound Vf has greater energy affinity binding values
(-12.898 kcal/mol) with 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase enzyme compared with
atorvastatin (-11.8605 kcal/mol). All synthesized compounds (Va-l) were able to decreases total cholesterol,
low-density lipoproteins and triglycerides and increased high-density lipoproteins and very low-density
lipoprotein in hyperlipidemic rats. Compounds Va-l have a good affinity towards 3-hydroxy-3-methyl-
glutaryl-coenzyme A reductase enzyme. High yield, good affinity, a nontoxic and low cardiac risk with
potential antihyperlipidemic activity make these compounds the possible lead for future research.
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