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dc.creatorAleksic, Ivana
dc.creatorJeremić, Jelena
dc.creatorMilivojevic, Dusan
dc.creatorIlić-Tomić, Tatjana
dc.creatorŠegan, Sandra
dc.creatorZlatović, Mario
dc.creatorOpsenica, Dejan
dc.creatorSenerovic, Lidija
dc.date.accessioned2019-11-05T09:39:58Z
dc.date.available2019-11-05T09:39:58Z
dc.date.issued2019
dc.identifier.issn1554-8929
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/3198
dc.description.abstractPseudomonas aeruginosa is a leading cause of nosocomial infections that are becoming increasingly difficult to treat due to the occurrence of antibiotic resistant strains. Since P. aeruginosa virulence is controlled through quorum sensing, small molecule treatments inhibiting quorum sensing signaling pathways provide a promising therapeutic option. Consequently, we synthesized a series of N-octaneamino-4-aminoquinoline derivatives to optimize this chemotype’s antivirulence activity against P. aeruginosa via inhibition of pyocyanin production. The most potent derivative, which possesses a benzofuran substituent, provided effective inhibition of pyocyanin production (IC50 = 12 μM), biofilm formation (BFIC50 = 50 μM), and motility. Experimentally, the compound’s activity is achieved through competitive inhibition of PqsR, and structure–activity data were rationalized using molecular docking studies.sr
dc.language.isoensr
dc.publisherAmerican Chemical Societysr
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS//sr
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/173048/RS//sr
dc.rightsrestrictedAccesssr
dc.sourceACS Chemical Biologysr
dc.subjectLong-Chained 4-Amino-7-chloro-quionolinessr
dc.subjectPseudomonas aeruginosasr
dc.subjectquorum sensingsr
dc.subjectInhibitors of Pyocyaninsr
dc.titleN-benzyl derivatives of long-chained 4-Amino-7-chloro-quionolines as inhibitors of pyocyanin production in Pseudomonas aeruginosasr
dc.typearticlesr
dc.rights.licenseARRsr
dcterms.abstractОпсеница, Дејан; Шеган, Сандра; Илиц-Томиц, Татјана; Миливојевиц, Дусан; Јеремиц, Јелена; Aлексиц, Ивана; Сенеровиц, Лидија; Златовић, Марио;
dc.rights.holderAmerican Chemical Societysr
dc.citation.volume14
dc.citation.issue12
dc.citation.spage2800
dc.citation.epage2809
dc.citation.rankM21~
dc.description.otherThe peer-reviewed version: [http://cer.ihtm.bg.ac.rs/handle/123456789/3341]
dc.identifier.pmid31647218
dc.identifier.doi10.1021/acschembio.9b00682
dc.identifier.scopus2-s2.0-85074933821
dc.identifier.wos000504806100033
dc.type.versionpublishedVersionsr


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