Journal article Open Access

NOVEL PENTA- SUBSTITUTED PYRIDINE NUCLEUS WITH PYRAZOLE ANALOGUES: MICROWAVE ASSISTED SYNTHESIS, DOCKING AND BIOLOGICAL SCREENING

Rahul P. Thummar*, Ronak D. Kamani, Nirav H. Sapariya, Beena K. Vaghasiya, Jemin R. Avalani and Dipak K. Raval

A novel series of 5-(4-formyl substituted phenoxy)-3-methyl-1-phenyl-1H-pyrazole-4-carbonitrile (1a-b) based penta-substituted pyridine derivatives 4(a–n) was synthesized by piperidine catalyzed cyclocondensation reaction through microwave. The newly synthesized compounds were characterized by spectral studies and also by C, H and N analyses. The synthesized compounds were tested for their in vitro tuberculosis activity against H37Rv strains using rifampicin, isoniazide and ethambutol as the standard drugs. All novel synthesized compounds were tested for their in vitro antimalarial activity against P. falciparum strains using quinine and chloroquine as the standard drugs. Molecular docking and pharmacokinetic study were carried out for all the targeted compounds. Keywords: - antimalarial activity, antituberculosis, docking, microwave assisted, pyridine

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