The synthesis of a novel series of 1,3,5-trisubstitiuted pyrazoline was achieved by refluxing
chalcone derivative with different heteroaryl hydrazines. The newly synthesized compounds were
characterized by 1H NMR, 13CNMR, mass spectral and elemental analysis data. The synthetic series of
novel pyrazoline hybrids was screened for in vitro schizont maturation assay against chloroquine sensitive
3D7 strain of Plasmodium falciparum. Most of the compounds showed promising in vitro antimalarial
activity against CQ sensitive strain. The preliminary structure-activity relationship study showed
that quinoline substituted analog at position N-1 showed maximum activity followed by benzothiazole
substitution, while phenyl substitution lowers the antimalarial activity. The observed activity was persistent
by the docking study on P. falciparum cystein protease falcipain-2. The pharmacokinetic properties
were also studied using ADME prediction.
