Pyrazinamide and pyrazinoic acid derivatives directed to mycobacterial enzymes against tuberculosis

Pyrazinamide and pyrazinoic acid derivatives directed to mycobacterial enzymes against tuberculosis

Author Correa, Michelle Fidelis Autor UNIFESP Google Scholar
Fernandes, Joao Paulo dos Santos Autor UNIFESP Google Scholar
Abstract Tuberculosis (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.
Keywords Antimycobacterial Agents
Drug Design
Prodrugs
Pyrazinamide
Pyrazinoic Acid
Resistant TbVitro Antimycobacterial Activity
Nadph Binding
Synthase I
Esters
Prodrugs
Analogs
Agent
Language English
Date 2016
Published in Current Protein & Peptide Science. Sharjah, v. 17, n. 3, p. 213-219, 2016.
ISSN 1389-2037 (Sherpa/Romeo, impact factor)
Publisher Bentham science publ ltd
Extent 213-219
Origin http://dx.doi.org/10.2174/1389203716666151002114839
Access rights Closed access
Type Revisão
Web of Science ID WOS:000372549600002
URI http://repositorio.unifesp.br/handle/11600/49570

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