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Benzofuroxan Derivatives as Potent Agents against Multidrug-Resistant Mycobacterium tuberculosis

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dc.contributor.authorFernandes, Guilherme F. S. [UNESP]
dc.contributor.authorCampos, Débora L. [UNESP]
dc.contributor.authorDa Silva, Isabel C. [UNESP]
dc.contributor.authorPrates, João L. B. [UNESP]
dc.contributor.authorPavan, Aline R. [UNESP]
dc.contributor.authorPavan, Fernando R. [UNESP]
dc.contributor.authorDos Santos, Jean L. [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2021-06-25T11:11:25Z
dc.date.available2021-06-25T11:11:25Z
dc.date.issued2021-04-20
dc.description.abstractTuberculosis (TB) is currently the leading cause of death related to infectious diseases worldwide, as reported by the World Health Organization. Moreover, the increasing number of multidrug-resistant tuberculosis (MDR-TB) cases has alarmed health agencies, warranting extensive efforts to discover novel drugs that are effective and also safe. In this study, 23 new compounds were synthesized and evaluated in vitro against the drug-resistant strains of M. tuberculosis. The compound 6-((3-fluoro-4-thiomorpholinophenyl)carbamoyl)benzo[c][1,2,5]oxadiazole 1-N-oxide (5 b) was particularly remarkable in this regard as it demonstrated MIC90 values below 0.28 μM against all the MDR strains evaluated, thus suggesting that this compound might have a different mechanism of action. Benzofuroxans are an attractive new class of anti-TB agents, exemplified by compound 5 b, with excellent potency against the replicating and drug-resistant strains of M. tuberculosis.en
dc.description.affiliationSchool of Pharmaceutical Sciences São Paulo State University (UNESP), Araraquara Jaú Highway KM 01
dc.description.affiliationInstitute of Chemistry São Paulo State University (UNESP), Francisco Degni Street 55
dc.description.affiliationUnespSchool of Pharmaceutical Sciences São Paulo State University (UNESP), Araraquara Jaú Highway KM 01
dc.description.affiliationUnespInstitute of Chemistry São Paulo State University (UNESP), Francisco Degni Street 55
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipIdFAPESP: 2016/09502-7
dc.description.sponsorshipIdFAPESP: 2018/00163-0
dc.description.sponsorshipIdFAPESP: 2018/11079-0
dc.description.sponsorshipIdFAPESP: 2018/17739-2
dc.description.sponsorshipIdFAPESP: 2018/21778-3
dc.description.sponsorshipIdFAPESP: 2018/24783-8
dc.description.sponsorshipIdCNPq: 404181/2019-8
dc.description.sponsorshipIdCNPq: 429139/2018-7
dc.format.extent1268-1282
dc.identifierhttp://dx.doi.org/10.1002/cmdc.202000899
dc.identifier.citationChemMedChem, v. 16, n. 8, p. 1268-1282, 2021.
dc.identifier.dimensionspub.1134397191
dc.identifier.doi10.1002/cmdc.202000899
dc.identifier.issn1860-7187
dc.identifier.issn1860-7179
dc.identifier.orcid0000-0002-4932-7720
dc.identifier.orcid0000-0003-2250-8342
dc.identifier.orcid0000-0002-2460-2829
dc.identifier.orcid0000-0002-0227-5054
dc.identifier.orcid0000-0002-6969-3963
dc.identifier.orcid0000-0001-9617-9858
dc.identifier.orcid0000-0003-0187-4626
dc.identifier.pmid33410233
dc.identifier.scopus2-s2.0-85100702147
dc.identifier.urihttp://hdl.handle.net/11449/208395
dc.language.isoeng
dc.publisherWiley
dc.relation.ispartofChemMedChem
dc.rights.accessRightsAcesso abertopt
dc.rights.sourceRightsoa_all
dc.rights.sourceRightsgreen
dc.sourceScopus
dc.sourceDimensions
dc.subjectantitubercular agents
dc.subjectbenzofuroxan
dc.subjectmultidrug-resistant TB
dc.subjectN-oxide
dc.subjecttuberculosis
dc.titleBenzofuroxan Derivatives as Potent Agents against Multidrug-Resistant Mycobacterium tuberculosisen
dc.typeArtigopt
dspace.entity.typePublication
relation.isDepartmentOfPublication5004bcab-94af-4939-b980-091ae9d0a19e
relation.isDepartmentOfPublication.latestForDiscovery5004bcab-94af-4939-b980-091ae9d0a19e
unesp.author.orcid0000-0002-7644-5466[1]
unesp.departmentCiências Biológicas - FCFpt

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Araraquara - FCF - Faculdade de Ciências Farmacêuticas