A new series of 4‐(4‐(1‐benzyl‐1H‐1,2,3‐triazol‐4‐yl)‐1‐phenyl‐1H‐pyrazol‐3‐yl)quinoline (6a‐t) have been synthesized by a click reaction of 4‐(4‐ethynyl‐1‐phenyl‐1H‐pyrazol‐3‐yl)quinoline (4a‐d) with a substituted benzyl azide (5a‐e). The starting alkyne derivatives 4a‐d are obtained from Bestmann‐Ohira reaction of 1‐phenyl‐3‐(quinolin‐4‐yl)‐1H‐pyrazole‐4‐carbaldehyde and dimethyl(1‐diazo‐2‐oxopropyl)phosphonate. The newly synthesized compounds are screened against M. tuberculosis H37Ra dormant and active, Escherichia coli, Pseudomonas fluorescence, Staphylococcus aureus and Bacillus subtilis strains at 30 μg/mL concentration. Most of the screened compounds showed good to moderate antibacterial activity against S. aureus, B. subtilis, and Mycobacterium tuberculosis H37Ra strains. The synthesized derivatives of quinolinyl‐pyrazole‐4‐carbaldehyde and quinolinyl‐pyrazole‐4‐ethyne reportd good to moderate activity against both strains of M. tuberculosis H37Ra. Ten derivatives of quinolinyl‐pyrazole presented good activity against B. subtilis. These results suggested that further optimization and development of quinolinyl‐pyrazolyl‐1,2,3‐triazole moeity could serve as lead compounds for antimycobacterial activity.

Microbial infections remain a grave threat to global health security due to an increase in antibiotic resistance. The ongoing coronavirus pandemic has increased the risk of microbial and fungal infections....

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