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5-Hydrazinylethylidenepyrimidines effective against multidrug-resistant Acinetobacter baumannii: Synthesis and in vitro biological evaluation of antibacterial, radical scavenging and cytotoxic activities

2019Journal article Restricted access
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dc.contributor.authorFigueiredo, Joana
dc.contributor.authorSerrano, João L.
dc.contributor.authorSoares, MN
dc.contributor.authorFerreira, Susana
dc.contributor.authorDomingues, F.C.
dc.contributor.authorAlmeida, Paulo
dc.contributor.authorSilvestre, Samuel
dc.date.accessioned2020-01-29T11:50:36Z
dc.date.available2020-01-29T11:50:36Z
dc.date.issued2019
dc.description.abstractAcinetobacter baumannii has emerged as an important nosocomial pathogen in recent years, with infectious outbreaks caused by multidrug-resistant strains increasing worldwide. Thus, new antibacterial treatments for multidrug-resistant A. baumannii strains are needed. In this work, a series of 5-hydrazinylethylidenepyrimidines were synthesized and in vitro evaluated against two multidrug-resistant A. baumannii strains (AcB 13/10 and AcB 73/10). Minimum inhibitory concentration results demonstrated that generally the compounds in study presented values in a low micromolar range. In the determination of in vitro bacterial growth at 24 h, it was observed that the pyrimidines 3a and 3c, with an unsubstituted hydrazinylphenyl, have bacteriostatic activity in both multidrug-resistant A. baumannii strains, with a concentration-dependent action. In general, an additive effect occurred in the combination of these compounds with gentamicin, rifampicin and polymyxin B, for both strains. Furthermore, all 5-hydrazinylethylidenepyrimidines under study presented a good 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity, generally low xanthine oxidase inhibition and low cytotoxicity in normal human dermal fibroblasts as well as potential favorable drug-likeness properties. Thus, these molecules can be considered attractive for the future development of antibacterial agents against multidrug-resistant A. baumannii.pt_PT
dc.description.sponsorshipSantander-Totta/UBI (BID/ICI-UID FC/Santander Universidades-UBI/2017pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.doi10.1016/j.ejps.2019.104964pt_PT
dc.identifier.urihttp://hdl.handle.net/10400.6/8880
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherElsevierpt_PT
dc.relation.publisherversionhttps://www.sciencedirect.com/science/article/pii/S0928098719302271?via%3Dihubpt_PT
dc.subject5-hydrazinylethylidenepyrimidinespt_PT
dc.subjectAntibacterial effectspt_PT
dc.subjectMultidrug-resistant A. baumanniipt_PT
dc.subjectXanthine oxidase inhibitionpt_PT
dc.subjectAntioxidant activitypt_PT
dc.subjectCytotoxicitypt_PT
dc.title5-Hydrazinylethylidenepyrimidines effective against multidrug-resistant Acinetobacter baumannii: Synthesis and in vitro biological evaluation of antibacterial, radical scavenging and cytotoxic activitiespt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876/UID%2FMulti%2F00709%2F2013/PT
oaire.citation.startPage104964pt_PT
oaire.citation.titleEuropean Journal of Pharmaceutical Sciencespt_PT
oaire.citation.volume137pt_PT
oaire.fundingStream5876
person.familyNameRodrigues Figueiredo
person.familyNameNeto Soares
person.familyNameFerreira
person.familyNameDomingues
person.familyNameAlmeida
person.familyNameSilvestre
person.givenNameJoana Patrícia
person.givenNameMafalda
person.givenNameSusana
person.givenNameFernanda
person.givenNamePaulo
person.givenNameSamuel
person.identifier.ciencia-id5C1D-F8C1-505C
person.identifier.ciencia-id4A19-FB45-BD67
person.identifier.ciencia-idF718-3569-E911
person.identifier.ciencia-id6514-0498-3E8F
person.identifier.ciencia-id6E18-3C6F-6842
person.identifier.ciencia-id4711-9D77-F772
person.identifier.orcid0000-0002-4711-107X
person.identifier.orcid0000-0003-4777-7573
person.identifier.orcid0000-0001-8308-2862
person.identifier.orcid0000-0002-9540-0853
person.identifier.orcid0000-0003-0110-4795
person.identifier.orcid0000-0003-4297-5108
person.identifier.ridA-6810-2016
person.identifier.ridN-7295-2013
person.identifier.ridA-1600-2014
person.identifier.ridA-4822-2017
person.identifier.scopus-author-id34874668400
person.identifier.scopus-author-id10139481400
person.identifier.scopus-author-id7102848111
person.identifier.scopus-author-id8234535800
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.embargofctCopyright cedido à editora no momento da publicaçãopt_PT
rcaap.rightsclosedAccesspt_PT
rcaap.typearticlept_PT
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