Synthesis and antimalarial potential of some novel quinoline-pyrazolopyridine derivatives

Abstract

A series of 1-(4-methylquinolin-2-yl)-4,6-diaryl-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives was synthesized by the reaction of 3-cinnamoyl-4-hydroxy-6-methyl-2H-pyran-2-ones with 2-chloro-4,6-diphenylnicotinonitrile analogues in the presence of 2-hydrazino-4-methyl quinoline and ethanol. The newly synthesized compounds were characterized by IR, 1H NMR and mass spectral data. The synthetic series of novel quinolinepyrazolopyridine hybrids were screened for in vitro schizont maturation assay against chloroquine sensitive 3D7 strain of Plasmodium falciparum, from which the most five active analogues were further evaluated for in vivo 4-day suppressive test in Swiss albino mice. Among the series, 5p (containing 4-Cl substituent attached to both aryl ring) portrayed considerable potent antimalarial activity during in vitro as well as in vivo study