SYNTHESIS OF SUBSTITUTED 2-PYRAZOLINES AS POTENTIAL ANTIMALARIAL AGENTS

Abstract

A series of substituted 2-pyrazolines derivatives were synthesized by refluxing from various substituted chalcones and nicotinic acid hydrazide in two steps. Compounds were confirmed by physical and spectral data such as M.P., Rf, elemental analyses, IR, 1H NMR and Mass spectral data and were evaluated for antimalarial activity against chloroquinesensitive (MRC-2) and chloroquine-resistant (RKL-9) P. falciparum strains. Compounds 4d (IC50=0.050 μM for MRC-2 and IC =0.413 μM for RKL-9) displayed better antiplasmodial activity than the chloroquine. The in vitro cytotoxicity study conducted on the human HepG2 cell line (>30μM) and showed good selectivity index.