抗菌钢琴粪便和多吡啶Ru（II）配合物与噻唑肼基-铬-2,4-二酮：互变异构、膜破坏和电子传递干扰。

IF 2.6 4区生物学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

ChemBioChem Pub Date : 2025-04-11 DOI:10.1002/cbic.202401025

Fatlinda Rahmani, Gozde Demirci, Youri Cortat, Aurélien Crochet, Fabio Zobi

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引用次数: 0

摘要

合成了一种含有噻唑肼基-铬-2,4-二酮的（氮- 6-对伞花烃）Ru（II）和Ru（II）双双比配合物库，对其进行了表征，并对其抑菌活性和细胞毒性进行了评价。从这个文库中，一些化合物被鉴定为对耐甲氧西林金黄色葡萄球菌和甲氧西林敏感金黄色葡萄球菌有活性。多吡啶配合物的最低抑制浓度为3.1 μm，对健康真核细胞无毒性，治疗指数为bbb32。活性配合物似乎通过影响细菌膜的通透性和/或电子传递链来发挥其抗生素活性。

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Antimicrobial Piano-Stool and Polypyridyl Ru(II) Complexes with Thiazolhidrazinylidene-Chroman-2,4-Dione: Tautomerism, Membrane Disruption, and Electron Transport Interference.

A library of (η⁶-p-cymene)Ru(II) and Ru(II) bis-bpy complexes bearing thiazolhidrazinylidene-chroman-2,4-dione was synthesized, characterized, and the molecules are evaluated for their antibacterial activity and cytotoxicity. From this library, several compounds are identified as being active against Methicillin-resistant Staphylococcus aureus and Methicillin-sensitive S. aureus. A polypyridyl complex showed a noteworthy minimum inhibitor concentration of 3.1 μm and no toxicity in healthy eukaryotic cells with a therapeutic index of >32. Active complexes appear to exert their antibiotic activity by affecting both the permeabilization of the bacterial membrane and/or the electron transport chain.

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来源期刊

ChemBioChem 生物-生化与分子生物学

CiteScore

6.10

自引率

3.10%

发文量

407

审稿时长

1 months

期刊介绍： ChemBioChem (Impact Factor 2018: 2.641) publishes important breakthroughs across all areas at the interface of chemistry and biology, including the fields of chemical biology, bioorganic chemistry, bioinorganic chemistry, synthetic biology, biocatalysis, bionanotechnology, and biomaterials. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies, and supported by the Asian Chemical Editorial Society (ACES).