Chimeric Amphiphilic Disinfectants: Quaternary Ammonium/Quaternary Phosphonium Hybrid Structures.
ChemMedChem
; 19(11): e202300718, 2024 Jun 03.
Article
em En
| MEDLINE
| ID: mdl-38416542
ABSTRACT
Cationic biocides play a crucial role in the disinfection of domestic and healthcare surfaces. Due to the rise of bacterial resistance towards common cationic disinfectants like quaternary ammonium compounds (QACs), the development of novel actives is necessary for effective infection prevention and control. Toward this end, a series of 15 chimeric biscationic amphiphilic compounds, bearing both ammonium and phosphonium residues, were prepared to probe the structure and efficacy of mixed cationic ammonium-phosphonium structures. Compounds were obtained in two steps and good yields, with straightforward and chromatography-free purifications. Antibacterial activity evaluation of these compounds against a panel of seven bacterial strains, including two MRSA strains as well as opportunistic pathogen A. baumannii, were encouraging, as low micromolar inhibitory activity was observed for multiple structures. Alkyl chain length on the ammonium group was, as expected, a major determinant of bioactivity. In addition, high therapeutic indexes (up to 125-fold) for triphenyl phosphonium-bearing amphiphiles were observed when comparing antimicrobial activity to mammalian cell lysis activity.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Compostos Organofosforados
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Testes de Sensibilidade Microbiana
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Desinfetantes
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Compostos de Amônio Quaternário
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Antibacterianos
Limite:
Humans
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article