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Synthesis, Characterization, Molecular Modelling and Biological Evaluation of Substituted Benzo (h) Chromene-3-Carboxylate Derivatives as a Potential Agent for the Treatment of Hyperlipidemia

Author(s): V. S. Verma, H. R. Badwaik*, Y. Vaishnav, A. Alexander and Ajazuddin
Faculty of Pharmaceutical sciences, Shri Shankaracharya Technical Campus, Bhilai 490020, 1Rungta College of Pharmaceutical Sciences and Research, Bhilai 490024, Chhattisgarh, 2National Institute of Pharmaceutical Education and Research, Guwahati 781101, Assam, 3Department of Pharmaceutics, School of Pharmacy and Technology Management, SVKM’s NMIMS, Shirpur 425405, Maharashtra, India

Correspondence Address:
H. R. Badwaik, Rungta College of Pharmaceutical Sciences and Research, Bhilai 490024, Chhattisgarh, India, E-mail:

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-methylglutaryl- 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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