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Organic salts based on isoniazid drug: Synthesis, bioavailability and cytotoxicity studies

dc.contributor.authorSantos, Filipa
dc.contributor.authorBranco, Luís C.
dc.contributor.authorDuarte, Ana Rita C.
dc.contributor.institutionLAQV@REQUIMTE
dc.contributor.institutionDQ - Departamento de Química
dc.contributor.pblMDPI AG
dc.date.accessioned2021-07-19T22:17:57Z
dc.date.available2021-07-19T22:17:57Z
dc.date.issued2020-10-10
dc.descriptionUIDB/50006/2020 POCI-01-0145-FEDER?007265 PTDC/QUI-QOR/32406/2017 MAR-02.01.01-FEAMP-0042
dc.description.abstractTuberculosis is one of the ten causes of morbidity and mortality worldwide caused by Mycobacterium tuberculosis complex. Some of the anti-tuberculosis drugs used in clinic studies, despite being effective for the treatment of tuberculosis, present serious adverse effects as well as poor bioavailability, stability, and drug-resistance problems. Thus, it is important to develop approaches that could provide shorter drug regimens, preventing drug resistance, toxicity of the antibiotics, and improve their bioavailability. Herein, we reported the use of organic salts based on the isoniazid drug, which can act as an organic cation combined with suitable organic anions such as alkylsulfonate-based (mesylate, R or S-Camphorsulfonate), carboxylate-based (glycolate, vanylate) and sacharinate. The synthesis, characterization, and cytotoxicity studies comparing with the original isoniazid drug have been performed. The possibility to explore dicationic salts seems promising in order to improve original bioavailability, and promote the elimination of polymorphic forms as well as higher stability, which are relevant characteristics that the pharmaceutical industry pursues.en
dc.description.versionpublishersversion
dc.description.versionpublished
dc.format.extent15
dc.format.extent1360536
dc.identifier.doi10.3390/pharmaceutics12100952
dc.identifier.issn1999-4923
dc.identifier.otherPURE: 32646123
dc.identifier.otherPURE UUID: d06af9cb-c1a7-4820-aa29-798fbd216aa7
dc.identifier.otherScopus: 85092474103
dc.identifier.otherPubMed: 33050373
dc.identifier.otherPubMedCentral: PMC7600673
dc.identifier.otherWOS: 000587425200001
dc.identifier.otherORCID: /0000-0003-0800-0112/work/97208912
dc.identifier.urihttp://hdl.handle.net/10362/121299
dc.identifier.urlhttps://www.scopus.com/pages/publications/85092474103
dc.language.isoeng
dc.peerreviewedyes
dc.relationinfo:eu-repo/grantAgreement/EC/H2020/725034/EU
dc.relationWhen solids become liquids: natural deep eutectic solvents for chemical process engineering
dc.relationSupport for European Aeronautical SMEs
dc.subjectBioavailability
dc.subjectCytotoxicity
dc.subjectIonic liquids & organic salts
dc.subjectIsoniazid
dc.subjectTuberculosis
dc.subjectPharmaceutical Science
dc.subjectSDG 3 - Good Health and Well-being
dc.titleOrganic salts based on isoniazid drug: Synthesis, bioavailability and cytotoxicity studiesen
dc.typejournal article
degois.publication.firstPage1
degois.publication.issue10
degois.publication.lastPage15
degois.publication.titlePharmaceutics
degois.publication.volume12
dspace.entity.typePublication
oaire.awardNumber725034
oaire.awardNumber200426
oaire.awardTitleWhen solids become liquids: natural deep eutectic solvents for chemical process engineering
oaire.awardTitleSupport for European Aeronautical SMEs
oaire.awardURIinfo:eu-repo/grantAgreement/EC/H2020/725034/EU
oaire.awardURIinfo:eu-repo/grantAgreement/EC/FP7/200426/EU
oaire.fundingStreamH2020
oaire.fundingStreamFP7
project.funder.identifierhttp://doi.org/10.13039/501100008530
project.funder.identifierhttp://doi.org/10.13039/501100008530
project.funder.nameEuropean Commission
project.funder.nameEuropean Commission
rcaap.rightsopenAccess
relation.isProjectOfPublicationc3c7a420-917d-40d1-8eee-26b6ad145ebd
relation.isProjectOfPublication2265f078-0bc6-44ac-a9dc-56e06854c27c
relation.isProjectOfPublication.latestForDiscoveryc3c7a420-917d-40d1-8eee-26b6ad145ebd

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