Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents

Abstract

To develop new antibacterial agents, a series of novel triazole-containing pyrazole ester derivatives were designed and synthesized and their biological activities were evaluated as potential topoisomerase II inhibitors. Compound 4d exhibited the most potent antibacterial activity with Minimum inhibitory concentration (MIC) alues of 4 µg/mL, 2 µg/mL, 4 µg/mL, and 0.5 µg/mL against Staphylococcus aureus, Listeria monocytogenes, Escherichia coli, and Salmonella gallinarum, respectively. The in vivo enzyme inhibition assay 4d displayed the most potent topoisomerase II (IC50 = 13.5 µg/mL) and topoisomerase IV (IC50 = 24.2 µg/mL) inhibitory activity. Molecular docking was performed to position compound 4d into the topoisomerase II active site to determine the probable binding conformation. In summary, compound 4d may serve as potential topoisomerase II inhibitor.

Synthesis, Crystal Structure, Antifungal Activity, and Docking Study of Difluoromethyl Pyrazole Derivatives

“…Pyrazole is an important five‐membered heterocycle, which can be found in many drugs or pesticides . In the recent years, lots of succinate dehydrogenase inhibitors contain pyrazole motif , such as penthiopyrad, sedaxane, pydiflumetofen, bixafen, isopyrazam, and pyrapropoyne fluxapyroxad.…”

Insights into idarubicin antimicrobial activity against methicillin-resistant Staphylococcus aureus

“…S. aureus DNA gyrase and 5× reaction buffer [40 mM Hepes KOH (pH 7.6), 500 mM potassium glutamate, 2 mM ATP, 0.05 mg/ml albumin, and 10 mM DTT] were obtained from Enzo Biochem (New York, America). The efficacy of DNA gyrase to supercoil relaxed DNA in the presence of ciprofloxacin (CIP, positive control) and IDAR was determined by gel electrophoresis [ 30 , 31 ].…”

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“…Several recent studies demonstrated drug resistance for their recommended antibiotic therapy with increasing prevalence in parasitic protozoa including Trypanosoma, Plasmodium, Toxoplasma gondii, Leishmania, and Entamoeba. [13][14][15][16] During the early stages of medicinal chemistry development, scientists were primarily concerned with the isolation of medicinal agents found in plants. Today, scientists in this field are also equally concerned with the creation of new synthetic drug compounds.…”