Inhibitory effect on biofilm formation of pathogenic bacteria induced by rubrolide lactam analogues

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dc.creatorAna Miranda
dc.creatorLuiz Cláudio de Almeida Barbosa
dc.creatorMohammed Masood
dc.creatorJodieh Varejão
dc.creatorMariane Sordi
dc.creatorCésar Benfatti
dc.creatorAndréa Pimenta
dc.date.accessioned2025-03-07T18:20:15Z
dc.date.accessioned2025-09-08T22:50:32Z
dc.date.available2025-03-07T18:20:15Z
dc.date.issued2018-12-27
dc.format.mimetypepdf
dc.identifier.doihttps://doi.org/10.1021/acsomega.8b02334
dc.identifier.issn2470-1343
dc.identifier.urihttps://hdl.handle.net/1843/80560
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofACS Publication
dc.rightsAcesso Aberto
dc.subjectAntibióticos
dc.subjectBiologia
dc.subjectBactéria
dc.subject.otherRubrolides
dc.subject.otherBiofilm inhibition
dc.subject.otherY-alkylidenebutenolides
dc.subject.otherAntibiotic
dc.titleInhibitory effect on biofilm formation of pathogenic bacteria induced by rubrolide lactam analogues
dc.typeArtigo de periódico
local.citation.epage18480
local.citation.issue12
local.citation.spage18475
local.citation.volume3
local.description.resumoA 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.
local.publisher.countryBrasil
local.publisher.departmentICX - DEPARTAMENTO DE QUÍMICA
local.publisher.initialsUFMG
local.url.externahttps://pubs.acs.org/doi/10.1021/acsomega.8b02334

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