Effects of synthetic tetronamides and methylated denigrins on bacterial quorum sensing and biofilm formation

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Tipo

Artigo de periódico

Título alternativo

Primeiro orientador

Membros da banca

Resumo

Detrimental biofilms of bacterial pathogens cause chronic infections with a high-level tolerance to antibiotics. To identify new control agents, we synthesized and tested a total of 14 tetronamides (including 5 new compounds) and 6 denigrin intermediates on the model species Escherichia coli. At a concentration of 50 μg/mL, two tetronamides and two methylated denigrins exhibited significant inhibitory effects against biofilm formation of E. coli RP437, e.g., by 60 and 94%, respectively. Structural analysis of the tested compounds revealed that p-methoxybenzylidene and p-methoxyphenethyl moieties of denigrins are important for biofilm inhibition, while the former group is also essential to the activity against quorum sensing (QS) via AI-2. Specifically, tetramethyldenigrin B has strong inhibitory effects against both E. coli biofilm formation and AI-2-mediated QS and thus provides a promising lead structure for designing better control agents. Consistently, tetramethyldenigrin B also showed inhibitory activity against biofilm formation of uropathogenic E. coli. Together, these findings provide new insights for the rational design of novel biofilm and QS inhibitors.

Abstract

Assunto

Patologia, Bactéria, Bactérias patogênicas, Biologia

Palavras-chave

Biofilm inhibition, Tetronamides, Denigrins, Butenolide

Citação

Curso

Endereço externo

https://pubs.acs.org/doi/10.1021/acsomega.3c01729

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