Pyrazinamide and pyrazinoic acid derivatives directed to mycobacterial enzymes against tuberculosis

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dc.contributor.authorCorrea, Michelle Fidelis [UNIFESP]
dc.contributor.authorFernandes, Joao Paulo dos Santos [UNIFESP]
dc.date.accessioned2019-01-21T10:30:05Z
dc.date.available2019-01-21T10:30:05Z
dc.date.issued2016
dc.description.abstractTuberculosis (TB) is an infectious diseases responsible for thousands of deaths worldwide. Due to the use of antimycobacterial drugs, TB prevalence seemed to be controlled, but with the appearance of resistant tuberculosis cases, the concern about the disease had become significant again, as well as the need for new alternatives to TB treatment. Since pyrazinamide (PZA) is part of the first-line agents in TB treatment, several derivatives of this drug were described, besides pyrazinoic acid (POA) derivatives, the active form of PZA. POA has been used mainly to design prodrugs to be activated by mycobacterial esterases, while PZA derivatives should be activated specifically by the nicotinamidase/ pyrazinamidase (PZAse), or other PZAse-independent pathways. The intention of this paper is to discuss the state of art of PZA and POA derivatives and their activity against Mycobacterium tuberculosis and other mycobacteria, besides the therapeutic potential. Focus was given in prodrugs and derivatives directed to mycobacterial enzymes involved in its activation or mechanism of action.en
dc.description.affiliationDepartamento de Ciências Exatas e da Terra, Universidade Federal de São Paulo, Rua São Nicolau 210, 2º andar, 09913-030 Centro, Diadema SP, Brazil
dc.description.affiliationUnifespDepartamento de Ciências Exatas e da Terra, Universidade Federal de São Paulo, Rua São Nicolau 210, 2º andar, 09913-030 Centro, Diadema SP, Brazil
dc.description.sourceWeb of Science
dc.format.extent213-219
dc.identifierhttp://dx.doi.org/10.2174/1389203716666151002114839
dc.identifier.citationCurrent Protein & Peptide Science. Sharjah, v. 17, n. 3, p. 213-219, 2016.
dc.identifier.doi10.2174/1389203716666151002114839
dc.identifier.issn1389-2037
dc.identifier.urihttp://repositorio.unifesp.br/handle/11600/49570
dc.identifier.wosWOS:000372549600002
dc.language.isoeng
dc.publisherBentham science publ ltd
dc.relation.ispartofCurrent Protein & Peptide Science
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.subjectAntimycobacterial Agentsen
dc.subjectDrug Designen
dc.subjectProdrugsen
dc.subjectPyrazinamideen
dc.subjectPyrazinoic Aciden
dc.subjectResistant TbVitro Antimycobacterial Activityen
dc.subjectNadph Bindingen
dc.subjectSynthase Ien
dc.subjectEstersen
dc.subjectProdrugsen
dc.subjectAnalogsen
dc.subjectAgenten
dc.titlePyrazinamide and pyrazinoic acid derivatives directed to mycobacterial enzymes against tuberculosisen
dc.typeinfo:eu-repo/semantics/review
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