Issue 47, 2016

Design, synthesis, and characterization of a fluoro substituted novel pyrazole nucleus clubbed with 1,3,4-oxadiazole scaffolds and their biological applications

Abstract

A novel series of compounds incorporating a fluoro substituted pyrazole nucleus clubbed with 1,3,4-oxadiazole scaffolds (7a–p) was synthesized in good yields (79–89%). The structures of all the compounds were confirmed using elemental analysis, IR, 1H NMR, and mass spectral data. The newly synthesized compounds were screened for their preliminary in vitro antibacterial activity against a panel of pathogenic strains of bacteria and fungi; for their antituberculosis activity against Mycobacterium tuberculosis H37Rv; and for their and antimalarial activity against Plasmodium falciparum. Compounds 7e, 7o, and 7h were found to possess promising antibacterial potency, while compounds 7c, 7h, and 7j demonstrated better potency against M. tuberculosis H37Rv compared with that of rifampicin. Compounds 7b, 7h, 7i, 7l, and 7o were found to possess excellent activity against a P. falciparum strain compared with quinine (IC50 = 0.826 μM).

Graphical abstract: Design, synthesis, and characterization of a fluoro substituted novel pyrazole nucleus clubbed with 1,3,4-oxadiazole scaffolds and their biological applications

Supplementary files

Article information

Article type
Paper
Submitted
16 Jan 2016
Accepted
10 Apr 2016
First published
12 Apr 2016

RSC Adv., 2016,6, 41532-41541

Author version available

Design, synthesis, and characterization of a fluoro substituted novel pyrazole nucleus clubbed with 1,3,4-oxadiazole scaffolds and their biological applications

S. C. Karad, V. B. Purohit, J. R. Avalani, N. H. Sapariya and D. K. Raval, RSC Adv., 2016, 6, 41532 DOI: 10.1039/C6RA01349J

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