Synthesis and antimalarial potential of some novel quinoline-pyrazolopyridine derivatives.
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 quinoline-pyrazolopyridine hybrids were screened forin vitroschizont maturation assay against chloroquine sensitive 3D7 strain ofPlasmodium falciparum, from which the most five active analogues were further evaluated forin vivo4-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 duringin vitroas well asin vivostudy.
Drug Discovery and Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar-125001.
Deepika
D
Saini
Drug Discovery and Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar-125001.
Sandeep
S
Jain
Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra 136119.
Ajay
A
Kumar
Department of Pharmaceutical Education and Research, Bhagat Singh Phool Mahila Vishwavidyalaya, Khanpur Kalan, Sonepat-131305.
Neelam
N
Jain
Plasmodium; antimalarial activity; cyanopyridine; pyrazolopyridine; quinoline