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具有潜在抗菌活性的双环吡唑啉的合成与生物学评价

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

作者信息

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

机构信息

Department of Surgical Sciences and Integrated Diagnostics, University of Genova, Viale Benedetto XV, 6, 16132, Genoa, Italy.

Department of Pharmacy, Section of Medicinal Chemistry, University of Genova, Viale Benedetto XV, 3, 16132, Genoa, Italy.

出版信息

ChemMedChem. 2025 Jul 18;20(14):e202500144. doi: 10.1002/cmdc.202500144. Epub 2025 May 27.

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 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.

摘要

报道了使用流动技术高效光化学合成双环吡唑啉及其随后对这些支架的抗菌评估。发现对包括不同葡萄球菌属和肠球菌属物种在内的一系列耐多药细菌菌株的最低抑菌浓度值低至0.5 - 4μg/mL。由卤代芳基环系统修饰的先导化合物似乎具有抑菌作用,并表现出优异的物理化学和药代动力学性质。由于预测毒性水平低且药物相似性高,因此这些双环吡唑啉有望作为抗菌物种进行进一步研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/03ab/12276031/7baf96e1b127/CMDC-20-e202500144-g001.jpg

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