受大自然启发的新型季铵盐化合物：合成、抗菌和抗生物膜活性。

IF 3.6 4区医学 Q2 CHEMISTRY, MEDICINAL ChemMedChem Pub Date : 2024-11-19 DOI:10.1002/cmdc.202400807

Liubov Muzychka, Diana Hodyna, Larysa Metelytsia, Oleg Smolii

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引用次数: 0

摘要

受从海绵中分离出的海洋化合物的启发，以及对新型有效抗菌剂需求的增加，设计并合成了具有长烷基链（C8-C12）的新型季铵盐化合物。评估了新化合物对六种微生物菌株（金黄色葡萄球菌、大肠杆菌和绿脓杆菌）的抗菌和抗生物膜活性。所有合成的铵盐都具有抗菌活性，其 MIC 值在 5.0 至 25.0 μg/mL 之间。此外，大多数化合物在浓度为 5.0 μg/mL 时对金黄色葡萄球菌 ATCC 25923、铜绿假单胞菌 PA01 和耐可乐定铜绿假单胞菌（CRPA）的生物膜形成有很强的抑制作用。除耐药金黄色葡萄球菌（CRSA）外，铵盐 3 对所有测试的细菌生物膜都显示出 100% 的抑制活性。

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Nature-Inspired Novel Quaternary Ammonium Compounds: Synthesis, Antibacterial and Antibiofilm Activity.

Inspired by marine compounds isolated from sponges and the increased need for new effective antimicrobials, novel quaternary ammonium compounds with long alkyl chains (C8-C12) were designed and synthesized. Antibacterial and antibiofilm activity of new compounds was evaluated against six microbial strains (S. aureus, E. coli, and P. aeruginosa). All synthesized ammonium salts displayed antibacterial activity with MIC values ranging from 5.0 to 25.0 μg/mL. In addition, most compounds showed strong inhibition of biofilm formation of S. aureus ATCC 25923, P. aeruginosa PA01, and colistin-resistant P. aeruginosa (CRPA) at a concentration of 5.0 μg/mL. Ammonium salt 3 showed 100% inhibitory activity against all tested bacterial biofilms except that of colistin-resistant S. aureus (CRSA).

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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

期刊介绍： Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs. Contents ChemMedChem publishes an attractive mixture of: Full Papers and Communications Reviews and Minireviews Patent Reviews Highlights and Concepts Book and Multimedia Reviews.