SYNTHESIS AND BIOLOGICAL EVALUATION OF 1,3,5-TRISUBSTITUTED PYRAZOLINES AS ANTIMALARIAL–ANTIMICROBIAL AGENTS

A convenient and efficient reaction of chalcone for the synthesis of highly functionalized pyrazole and pyridine has been developed. Many pieces of evidence point out the relevance of natural compounds for malaria and its prevention, including chalcones. Ring substituted quinolines are synthesized as the emerging class of antimalarial agents. Two series i.e. 4-(3-(substituted phenyl)-5-(2,6-dichloroquinolin-3-yl)-4, 5-dihydro-1H-pyrazol-1-yl)benzene sulfonamide (4a-4e) and [5-(2,6-dichloroquinolin-3-yl)-3-(substituted phenyl)-4,5-dihydro-1H-pyrazol-1-yl]pyridine-3-yl-methanone.(4a'-4e') were synthesized. Above mentioned compounds were characterized by FTIR, 1H-NMR, 13C-NMR, mass spectrometry and elemental analysis. Attempt has been made to investigate the mechanism behind the formation of substituted quinolines. All the synthesized substituted quinolines have shown moderate to good antimalarial activity and good antimicrobial activity against bacterial and fungal strains. Compounds 4a and 4d' were found to be the candidate compounds to investigate further for its potential antimalarial and antimicrobial activity.