Synthesis and antimalarial potential of some novel quinoline-pyrazolopyridine derivatives

Authors

  • Deepika Saini Drug Discovery and Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar-125001
  • Sandeep Jain Drug Discovery and Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar-125001
  • Ajay Kumar Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra 136119
  • Neelam Jain Department of Pharmaceutical Education and Research, Bhagat Singh Phool Mahila Vishwavidyalaya, Khanpur Kalan, Sonepat-131305

DOI:

https://doi.org/10.17179/excli2016-677

Keywords:

quinoline, pyrazolopyridine, cyanopyridine, antimalarial activity, Plasmodium

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 quinoline-pyrazolopyridine 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.

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Published

2016-11-28

How to Cite

Saini, D., Jain, S., Kumar, A., & Jain, N. (2016). Synthesis and antimalarial potential of some novel quinoline-pyrazolopyridine derivatives. EXCLI Journal, 15, 730–737. https://doi.org/10.17179/excli2016-677

Issue

Vol. 15 (2016)

Section

Original articles

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