Inhibitory effect on biofilm formation of pathogenic bacteria induced by rubrolide lactam analogues
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Universidade Federal de Minas Gerais
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Artigo de periódico
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Membros da banca
Resumo
A series of 32 novel potential bacterial biofilm inhibitor analogues of rubrolides and their lactam derivatives weresynthesized. The compounds were prepared and tested against Staphylococcus aureus and Staphylococcus epidermidis. In general,γ-alkylidene-γ-lactams are more active than the corresponding γ-alkylidene-γ-lactones, and the two derivatives are more effectivein inhibiting bacterial planktonic growth (IC50 of 1.8 and 5.6 μg mL−1) than natural rubrolides. Compounds showing little effecton planktonic growth were assayed for their ability to inhibit biofilm formation. As biofilm inhibitors, none of the newcompounds were effective against S. epidermidis, whereas the three Z-lactam derivatives were very active against S. aureus (IC 50 =0.9−3.3 μg mL−1). The strong antibiofilm formation activity displayed by some γ-alkylidene-γ-lactams indicates that this mayrepresent a promising class of compounds for the development of novel antimicrobial agents against clinically relevant Gram-positive bacteria.
Abstract
Assunto
Antibióticos, Biologia, Bactéria
Palavras-chave
Rubrolides, Biofilm inhibition, Y-alkylidenebutenolides, Antibiotic
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https://pubs.acs.org/doi/10.1021/acsomega.8b02334