The efficient photochemical synthesis of bicyclic pyrazolines using flow technology as well as the subsequent antimicrobial evaluation of these scaffolds is reported. Low MIC values of 0.5-4 μg/mL were found against a series of multidrug resistant bacterial strains including different Staphylococcus and Enterococcus genera. The lead compound, which is decorated by a halogenated aryl ring system, appears to be bacteriostatic and shows excellent physicochemical and pharmacokinetic properties. Due to low levels of predicted toxicity combined with a high level of drug-likeness, these bicyclic pyrazolines therefore are promising candidates for further studies as antibacterial species.
Synthesis and Biological Evaluation of Bicyclic Pyrazolines with Promising Antimicrobial Activities.
Caviglia D.;Schito A. M.;Penco S.;Brullo C.;
2025-01-01
Abstract
The efficient photochemical synthesis of bicyclic pyrazolines using flow technology as well as the subsequent antimicrobial evaluation of these scaffolds is reported. Low MIC values of 0.5-4 μg/mL were found against a series of multidrug resistant bacterial strains including different Staphylococcus and Enterococcus genera. The lead compound, which is decorated by a halogenated aryl ring system, appears to be bacteriostatic and shows excellent physicochemical and pharmacokinetic properties. Due to low levels of predicted toxicity combined with a high level of drug-likeness, these bicyclic pyrazolines therefore are promising candidates for further studies as antibacterial species.
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