受自然启发的新型季铵化合物：合成、抗菌及抗生物膜活性
Nature-inspired Novel Quaternary Ammonium Compounds: Synthesis, Antibacterial and Antibiofilm Activity.
作者信息
Muzychka Liubov, Hodyna Diana, Metelytsia Larysa, Smolii Oleg
机构信息
Department of Chemistry of Natural Compounds, V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine, 1 Academician Kukhar Str., 02094, Kyiv, Ukraine.
出版信息
ChemMedChem. 2025 Mar 3;20(5):e202400807. doi: 10.1002/cmdc.202400807. Epub 2024 Dec 2.
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).
受从海绵中分离出的海洋化合物以及对新型有效抗菌剂需求增加的启发，设计并合成了具有长烷基链（C8 - C12）的新型季铵化合物。针对六种微生物菌株（金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌）评估了新化合物的抗菌和抗生物膜活性。所有合成的铵盐均表现出抗菌活性，其最低抑菌浓度（MIC）值范围为5.0至25.0μg/mL。此外，大多数化合物在浓度为5.0μg/mL时对金黄色葡萄球菌ATCC 25923、铜绿假单胞菌PA01和耐黏菌素铜绿假单胞菌（CRPA）的生物膜形成具有强烈抑制作用。铵盐3对除耐黏菌素金黄色葡萄球菌（CRSA）外的所有测试细菌生物膜均表现出100%的抑制活性。
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