DESIGN, SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF PROPROTEIN CONVERTASE SUBSTILSIN/KEXIN TYPE 9 INHIBITORS AS POTENT ANTI-HYPERLIPIDEMIC AGENTS
AbstractHyperlipidemia is a systemic disease, which is characterized by elevated lipid levels in blood including total cholesterol (TC), total glyceride (TG), low density lipoprotein cholesterol (LDL-c) and so on. It is one of the major risk factors leading to fatty liver, cardiovascular diseases and atherosclerosis and become the first killer of human health. The present study involves synthesis of some novel heterocycles of benzoxazole derivatives containing Oxadiazole and amino triazole and its evaluation of in-vivo and in-silico molecular docking for determining antihyperlipidemic activity. The chemical structures of newly synthesized compounds were evaluated by spectrum of IR, 1HNMR, and LC-MS. The molecular docking studies for the synthesized compounds with PCSK9 showed energy levels ranging from -8 to -10kcal/mol. The compound VD1which shows least binding energy taken for in-vivo antihyperlipidemic activity study. The antihyperlipidemic activity was evaluated by high fat diet induced hyperlipidaemia model and the compound VD1 showed significant reduction in serum lipid parameters as that of standard drug Atorvastatin.
Article Information
11
2701-2708
1306 KB
208
English
IJPSR
R. Priyadarsini *, V. Dinesh Kumar and S. Abiseik
Department of Pharmaceutical Chemistry, College of Pharmacy, Madras Medical College, Chennai, Tamil Nadu, India.
rpdharsinimpharm@gmail.com
22 January 2024
09 August 2024
12 August 2024
10.13040/IJPSR.0975-8232.15(9).2701-08
01 September 2024
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