Synthesis and Biological Evaluation of Bicyclic Pyrazolines with Promising Antimicrobial Activities.

IF 3.6 4区医学 Q2 CHEMISTRY, MEDICINAL

ChemMedChem Pub Date : 2025-05-07 DOI:10.1002/cmdc.202500144

Debora Caviglia, Anna Maria Schito, Susanna Penco, Chiara Brullo, Marcus Baumann

引用次数: 0

Abstract

The efficient photochemical synthesis of bicyclic pyrazolines using flow technology as well as the subsequent antimicrobial evaluation of these scaffolds is reported. Low minimal inhibitory concentration values of 0.5-4 μg mL^-1 are found against a series of multidrug resistant bacterial strains including different Staphylococcus and Enterococcus genera species. 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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具有抗菌活性的双环吡唑啉类化合物的合成及生物学评价。

本文报道了利用流动技术高效光化学合成双环吡唑啉以及随后对这些支架的抗菌评价。对多种葡萄球菌和肠球菌属多重耐药菌株的MIC值均在0.5 ~ 4 μg/mL之间。先导化合物采用卤化芳基环修饰，具有抑菌作用，具有良好的理化和药动学性能。由于低水平的预测毒性加上高水平的药物相似性，这些双环吡唑啉因此是有希望进一步研究的抗菌物种。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

ChemMedChem 医学-药学

CiteScore

6.70

自引率

2.90%

发文量

280

审稿时长

1 months

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