Antimicrobial Efficacy of 1,2,3-Triazole-Incorporated Indole-Pyrazolone against Drug-Resistant ESKAPE Pathogens: Design and Synthesis.

In the current study, we report the synthesis of novel 4-((1-((1-1,2,3-triazole-4-yl)methyl)-1-indol-3-yl)methylene)-5-methyl-2-phenyl-2,4-dihydro-3-pyrazole-3-one derivatives -. The compounds were prepared through a Knoevenagel condensation reaction and copper-catalyzed azide-alkyne cycloaddition (CuAAC) Click chemistry approach. The synthesized compounds exhibited promising antimicrobial activity against both Gram-positive and Gram-negative bacteria. Compounds , , and displayed potent activity with MIC value against , in comparison to standard drugs chloramphenicol and ampicillin. Compounds , , , , and exhibited good-to-moderate antifungal activity against and equivalent to standard drugs nystatin and fluconazole. In this study, the cytotoxicity profile of a series of compounds was assessed using SHSY-5Y cells. The results indicate that compounds - exhibit no significant cytotoxicity at concentrations up to , in comparison to both untreated and vehicle control groups. These findings highlight the safety and tolerability of compounds as well as the potential of the synthesized compounds as effective agents against bacterial and fungal infections.