Publication:
Synthesis and Biological Activities of Some 1,3-Benzoxazol-2(3H)-One Derivatives as Anti-Quorum Sensing Agents

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dc.contributor.authorTINAZ, GÜLGÜN
dc.contributor.authorsMiandji, A. M.; Ulusoy, S.; Dundar, Y.; Ozgen, S.; Onurdag, F. K.; Bosgelmez-Tinaz, G.; Noyanalpan, N.
dc.date.accessioned2022-03-12T18:06:41Z
dc.date.available2022-03-12T18:06:41Z
dc.date.issued2012
dc.description.abstractAntibiotics are commonly used to treat microbial infections. Due to misuse or large-scale use of antibiotics, many pathogens have gained resistance which makes antibiotic treatments ineffective. The discovery that many bacteria use quorum sensing (QS) to regulate their virulence factor and pathogenicity production makes the QS system an attractive target for antimicrobial therapy. A series of 1,3-benzoxazol-2(3H)-one derivatives were designed and synthesized as QS inhibitors (QSIs) and tested for their QS inhibitory activities. In vitro quorum sensing inhibitor screen (QSIS) assay indicated that the 1,3-benzoxazol-2(3H)-one (compound 1), 5-chloro-1,3-benzoxazol-2(3H)-one (compound 6), 6-methyl-1,3-benzoxazol-2(3H)-one (compound 11), and 5-methyl-1,3-benzoxazol-2(3H)-one (compound 16), inhibit QS system in quorum sensing selector (QSIS)1 strain. These 4 QSIs also significantly reduced elastase production, biofilm formation and swarming motility of Pseudomonas aeruginosa PA01 strain. These results suggest that compound 1, 6, 11 and 16 may provide a starting point for the design and development of new anti-pathogenic drugs that restrict virulence of P. aeruginosa and possibly other clinically important human pathogens. In addition, these QSI molecules could potentially be used in combination with conventional antibiotics to increase the efficiency of disease control and to extend the life span of established antimicrobials.
dc.identifier.doi10.1055/s-0032-1312590
dc.identifier.eissn1616-7066
dc.identifier.issn0004-4172
dc.identifier.pubmed22588631
dc.identifier.urihttps://hdl.handle.net/11424/230939
dc.identifier.wosWOS:000307038800005
dc.language.isoeng
dc.publisherGEORG THIEME VERLAG KG
dc.relation.ispartofARZNEIMITTELFORSCHUNG-DRUG RESEARCH
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectacyl homoserine lactone
dc.subjectquorum sensing inhibitors
dc.subject1,3-benzoxazol-2(3H)-one
dc.subjectPSEUDOMONAS-AERUGINOSA
dc.subjectVIRULENCE
dc.subjectTOBRAMYCIN
dc.subjectINHIBITORS
dc.subjectSIGNALS
dc.subjectLUXR
dc.titleSynthesis and Biological Activities of Some 1,3-Benzoxazol-2(3H)-One Derivatives as Anti-Quorum Sensing Agents
dc.typearticle
dspace.entity.typePublication
local.avesis.idf566fec8-072b-4a7a-9124-c0ddb685c898
local.import.packageSS17
local.indexed.atWOS
local.indexed.atSCOPUS
local.journal.numberofpages5
oaire.citation.endPage334
oaire.citation.issue7
oaire.citation.startPage330
oaire.citation.titleARZNEIMITTELFORSCHUNG-DRUG RESEARCH
oaire.citation.volume62
relation.isAuthorOfPublication04cb59f2-2e4f-4b7f-b8f9-653ea79728d6
relation.isAuthorOfPublication.latestForDiscovery04cb59f2-2e4f-4b7f-b8f9-653ea79728d6

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