Synthesis and Antibacterial Evaluation of Bis-thiazolium, Bis-imidazolium, and Bis-triazolium Derivatives.
ChemMedChem
; 14(13): 1232-1237, 2019 07 03.
Article
em En
| MEDLINE
| ID: mdl-31115160
ABSTRACT
Given the worldwide spread of bacterial drug resistance, there is an urgent need to develop new compounds that exhibit potent antibacterial activity and that are unimpaired by this phenomenon. Quaternary ammonium compounds have been used for many years as disinfectants, but recent advances have shown that polycationic derivatives exhibit much stronger activity and are less prone to bacterial resistance than commonly used monocationic compounds. In this sense, we prepared three series of new bis-cationic compounds bis-thiazoliums, bis-imidazoliums, and bis-1,2,4-triazoliums. If some compounds of the first series showed fair antibacterial activity, most of those belonging to the two other series were highly potent, with minimum inhibitory concentrations close to 1â
µg mL-1 . Some of them also exhibited low toxicity toward eukaryotic MRC-5 lung fibroblasts, and we showed that this toxicity is clearly correlated with clogP. Finally, four selected compounds were found to exhibit a clear bactericidal effect.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tiazóis
/
Triazóis
/
Imidazóis
/
Antibacterianos
Limite:
Humans
Idioma:
En
Revista:
ChemMedChem
Assunto da revista:
FARMACOLOGIA
/
QUIMICA
Ano de publicação:
2019
Tipo de documento:
Article
País de afiliação:
França