Background: A range of biological activities including anti-inflammatory, antiangiogenic,
antitubercular and kinase inhibitory activity have been reported for pyrazole derivatives. Serious medicinal
chemistry approaches for the development of effective antibacterial agents have resulted in
only few new compounds with the lack of activity against a wide range of microbes. In continuation
with our quest for developing anti-inflammatory and antimicrobial agents bearing pyrazole scaffold, a
series of N-pyrazolylbenzamides 1-22 were synthesized.
Methods: All the desired compounds have been synthesized by following reported chemical reactions
and upon confirmation of structure of compounds through spectral data, all the compounds were
screened for antibacterial including resistant strains, antifungal, antitubercular activity and antiinflammatory
Results: In the antibacterial activity screening four compounds exhibited potent antibacterial activity
and admirable antifungal activity. Compounds 7 and 17 demonstrated potent activity with MIC of 3.12
µg/mL against Bacillus subtilis and compounds 3 and 17 were found to be highly potent against some
of resistant strains with MIC value of 3.12 µg/mL. Compounds 5 and 17 showed antitubercular activity
with MIC value of 6.25 µg/mL. All the compounds were also subjected for anti-inflammatory activity
at 50 mg/Kg dose, three compounds 8, 12 and 16 produced significant anti-inflammatory activity
over 50% in the third hour of observation.
Conclusion: Structurally characterized compounds have been screened for anti-inflammatory and antimicrobial
activities. Compounds 7 and 17 were found to be potent antibacterial compounds and 17
emerged out as one of the potent compounds with activity against MRSA, VRSA and E. faecium and
5 and 17 showed MIC value of 6.25 µg/mL against H37Rv mycobacterial strain. Compounds 4, 7, 8,
12 and 16 exhibited anti-inflammatory activity.