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Dihydropyrrolones as bacterial quorum sensing inhibitors.
Almohaywi, Basmah; Yu, Tsz Tin; Iskander, George; Chan, Daniel S H; Ho, Kitty K K; Rice, Scott; Black, David StC; Griffith, Renate; Kumar, Naresh.
Afiliación
  • Almohaywi B; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia; School of Pharmacy, King Khalid University Abha 62529, Saudi Arabia.
  • Yu TT; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Iskander G; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Chan DSH; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Ho KKK; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Rice S; The Singapore Centre of Environmental Life Sciences Engineering, Nanyang Technological University, Singapore 639798, Singapore.
  • Black DS; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Griffith R; Department of Pharmacology, School of Medical Sciences, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Kumar N; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia. Electronic address: n.kumar@unsw.edu.au.
Bioorg Med Chem Lett ; 29(9): 1054-1059, 2019 05 01.
Article en En | MEDLINE | ID: mdl-30857746
Bacteria regulate their pathogenicity and biofilm formation through quorum sensing (QS), which is an intercellular communication system mediated by the binding of signaling molecules to QS receptors such as LasR. In this study, a range of dihydropyrrolone (DHP) analogues were synthesized via the lactone-lactam conversion of lactone intermediates. The synthesized compounds were tested for their ability to inhibit QS, biofilm formation and bacterial growth of Pseudomonas aeruginosa. The compounds were also docked into a LasR crystal structure to rationalize the observed structure-activity relationships. The most active compound identified in this study was compound 9i, which showed 63.1% QS inhibition of at 31.25 µM and 60% biofilm reduction at 250 µM with only moderate toxicity towards bacterial cell growth.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pseudomonas aeruginosa / Pirroles Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Arabia Saudita Pais de publicación: Reino Unido
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pseudomonas aeruginosa / Pirroles Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Arabia Saudita Pais de publicación: Reino Unido