Authors : M. Singhal and A. Paul
Abstract: In the present study, researchers have used pharmacophore hybridization technique of drug design and designed a pharmacophore model chalconesemicarbazone which is having hydrogen acceptor site, hydrogen do nor site and lipophilic site, etc., using ligandscout-2.02 software. A series of 2-methyl pheny lsemicarbazone was synthesized and evaluated for their antipyretic activity using Brewe’s yeast induced pyrexia in rats. Based on the results of an antipyretic study, compound 12 was the most active compound. When the phenyl group of aldehydic and acetophenic moiety of chalcone is substituted with hydroxy group, the compounds exhibited better activity in comparison to substitution with the other groups like p-dimethyl amino groups. The unsubstituted compounds showed very less protection against pyrexia in comparison to the substituted compounds. The possible metabolites of some selected synthesized chalconesemicarbazones were predicted by computational method using Pallas Version-3.1 ADME-Tox prediction software. The major pathway of metabolism was found to be p-hydroxylation and amide hydrolysis.
M. Singhal and A. Paul, 2011. Synthesis Characterization and Antipyretic Evaluation of Some Novel Chalconesemicarbazone Derivatives. Research Journal of Pharmacology, 5: 47-52.