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In vitro assessment of antimicrobial, antioxidant, and cytotoxic properties of Saccharin-Tetrazolyl and-Thiadiazolyl derivatives: the simple dependence of the pH value on antimicrobial activity

2019Journal article Open access
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dc.contributor.authorFrija, Luís M. T.
dc.contributor.authorNtungwe, Epole
dc.contributor.authorSitarek, Przemysław
dc.contributor.authorAndrade, Joana M.
dc.contributor.authorToma, Monika
dc.contributor.authorŚliwiński, Tomasz
dc.contributor.authorCabral, Lília
dc.contributor.authorCristiano, Maria de Lurdes
dc.contributor.authorRijo, Patrícia
dc.contributor.authorPombeiro, Armando J. L.
dc.date.accessioned2020-03-02T15:38:18Z
dc.date.available2020-03-02T15:38:18Z
dc.date.issued2019
dc.description.abstractThe antimicrobial, antioxidant, and cytotoxic activities of a series of saccharin-tetrazolyl and -thiadiazolyl analogs were examined. The assessment of the antimicrobial properties of the referred-to molecules was completed through an evaluation of minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values against Gram-positive and Gram-negative bacteria and yeasts. Scrutiny of the MIC and MBC values of the compounds at pH 4.0, 7.0, and 9.0 against four Gram-positive strains revealed high values for both the MIC and MBC at pH 4.0 (ranging from 0.98 to 125 µg/mL) and moderate values at pH 7.0 and 9.0, exposing strong antimicrobial activities in an acidic medium. An antioxidant activity analysis of the molecules was performed by using the DPPH (2,2-diphenyl-1-picrylhydrazyl) method, which showed high activity for the TSMT (N-(1-methyl-2H-tetrazol-5-yl)-N-(1,1-dioxo-1,2-benzisothiazol-3-yl) amine, 7) derivative (90.29% compared to a butylated hydroxytoluene positive control of 61.96%). Besides, the general toxicity of the saccharin analogs was evaluated in an Artemia salina model, which displayed insignificant toxicity values. In turn, upon an assessment of cell viability, all of the compounds were found to be nontoxic in range concentrations of 0-100 µg/mL in H7PX glioma cells. The tested molecules have inspiring antimicrobial and antioxidant properties that represent potential core structures in the design of new drugs for the treatment of infectious diseases.pt_PT
dc.description.sponsorshipIST-ID/115/2018pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.doi10.3390/ph12040167pt_PT
dc.identifier.eissn1424-8247
dc.identifier.urihttp://hdl.handle.net/10400.1/13551
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.relation115/2018
dc.relationCentro de Química Estrutural
dc.relationMultifunctional Azole-based Frameworks for Dynamic Catalysis
dc.relationCentre of Marine Sciences
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectSaccharinpt_PT
dc.subjectTetrazolept_PT
dc.subject1, 3, 4-thiadiazolept_PT
dc.subjectH7PX glioma cellspt_PT
dc.subjectAntimicrobial screeningpt_PT
dc.subjectAntioxidant capacitypt_PT
dc.titleIn vitro assessment of antimicrobial, antioxidant, and cytotoxic properties of Saccharin-Tetrazolyl and-Thiadiazolyl derivatives: the simple dependence of the pH value on antimicrobial activitypt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleCentro de Química Estrutural
oaire.awardTitleMultifunctional Azole-based Frameworks for Dynamic Catalysis
oaire.awardTitleCentre of Marine Sciences
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FQUI%2F00100%2F2019/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT//SFRH%2FBPD%2F99851%2F2014/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FMulti%2F04326%2F2019/PT
oaire.citation.issue4pt_PT
oaire.citation.startPage167pt_PT
oaire.citation.titlePharmaceuticalspt_PT
oaire.citation.volume12pt_PT
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStream6817 - DCRRNI ID
person.familyNameCabral
person.familyNameCristiano
person.givenNameLília
person.givenNameMaria de Lurdes
person.identifier.ciencia-id3510-24A8-36B6
person.identifier.ciencia-idE411-6006-5A01
person.identifier.orcid0000-0001-9362-8128
person.identifier.orcid0000-0002-9447-2855
person.identifier.ridM-4279-2013
person.identifier.ridG-2345-2012
person.identifier.scopus-author-id9238724800
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublication175a6aa3-9993-480b-9663-ed083a17eedf
relation.isAuthorOfPublicationb16751a6-748e-44b0-9c59-058cbd5b2cc3
relation.isAuthorOfPublication.latestForDiscovery175a6aa3-9993-480b-9663-ed083a17eedf
relation.isProjectOfPublicationbe45ab2a-d999-4c52-8c31-4623cfce9018
relation.isProjectOfPublication0a29885b-8300-4d83-8d4c-a160d2f36a0d
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