Abstract
A series of bis-Mannich base derivatives of curcumin pyrazole (CP) have been synthesized and investigated for the potential of its anti-inflammatory activity in-vitro and in-silico. The synthesis was performed by aminomethylation of CP obtained from the cyclization of the 1,3-diketone chain of curcumin with hydrazine hydrate. The potential as an anti-inflammatory was accessed by the protein denaturation inhibition technique, and an in-silico study was performed against cyclooxygenase-1 and cyclooxygenase-2 via molecular docking. All the compounds showed better protein denaturation inhibitory activity than diclofenac sodium, curcumin, and CP used as standard and comparable compounds. Compound 2a exhibited the best active compound. The docking study found that the binding energy to COX-2 of all the compounds was lower than that of COX-1. The selectivity score (S) indicated that the compounds were very selective against COX-2. So, all the compounds possess high potential as anti-inflammatory agents, and further study is necessary to identify these compounds' safety and activity in- vivo.
Published Version
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