Pyrazinoic Acid
Mostrando 1-12 de 16 artigos, teses e dissertações.
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1. Anti-Sporothrix brasiliensis activity of different pyrazinoic acid prodrugs: a repurposing evaluation
From drug repurposing studies, this work aimed to evaluate the activity of different pyrazinoic acid (POA) derivatives against Sporothrix brasiliensis. The POA esters were prepared and characterized as previously reported by classical esterification reactions, with good to excellent yields. Sporothrix brasiliensis isolates from cats (n=6) and standard strain
Braz. J. Pharm. Sci.. Publicado em: 08/04/2019
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2. Evaluation of the influence of base and alkyl bromide on synthesis of pyrazinoic acid esters through fatorial design
Pyrazinoic acid esters have been synthesized as prodrugs of pyrazinoic acid. In the literature, its preparation is reported through the reaction of pyrazinoyl chloride with alcohols and the reaction with DCC/DMAP. In this work, it is reported a 2² factorial design to evaluate the preparation of these esters through the substitution of alkyl bromides with ca
Química Nova. Publicado em: 2009
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3. Synthesis and antimycobacterial activity of pyrazinoic acid esters and quinolones / Síntese e atividade antimicobacteriana de ésteres do ácido pirazinóico e quinolonas
Tuberculosis affects over than one billion people around the world. Since the discovery of rifampin, in 1965, no one another important drug was introduced in therapeutics. Pyrazinamide, one of the drugs available in therapy of tuberculosis, is nowadays considered a bioprecursor of pyrazinoic acid, because resistant bacterias do not express an enzyme, pyrazin
Publicado em: 2006
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4. Molecular characterization of pncA gene mutations in Brazilian Mycobacterium tuberculosis clinical isolates / "Caracterização molecular de mutações no gene pncA de isolados clínicos de Mycobacterium tuberculosis de origem brasileira"
Pyrazinamide (Z), a first-line antituberculous drug, is a prodrug that must be activated by bacterial pyrazinamidase (PZase) to the active form pyrazinoic acid, which kills M. tuberculosis. Many studies have shown that mutation in the gene encoding PZase (pncA) is the major mechanism of Z-resistance in M. tuberculosis. Based on this information and taking in
Publicado em: 2004
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5. Activity of n-propyl pyrazinoate against pyrazinamide-resistant Mycobacterium tuberculosis: investigations into mechanism of action of and mechanism of resistance to pyrazinamide.
The mechanism of action of pyrazinamide (PZA) is not known. One hypothesis is that PZA functions as a prodrug of pyrazinoic acid. Susceptibility to PZA correlates with amidase activity of the Mycobacterium tuberculosis isolate in question. PZA-resistant isolates retain susceptibility in vitro to pyrazinoic acid and n-propyl pyrazinoate. Esters of pyrazinoic
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6. Effects of Pyrazinamide on Fatty Acid Synthesis by Whole Mycobacterial Cells and Purified Fatty Acid Synthase I
The effects of low extracellular pH and intracellular accumulation of weak organic acids were compared with respect to fatty acid synthesis by whole cells of Mycobacterium tuberculosis and Mycobacterium smegmatis. The profile of fatty acids synthesized during exposure to benzoic, nicotinic, or pyrazinoic acids, as well as that observed during intracellular h
American Society for Microbiology.
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7. In vitro antimycobacterial activities of pyrazinamide analogs.
We synthesized various pyrazine derivatives and pyrazinamide analogs and assayed their antimycobacterial activities in vitro in order to find new drugs which are more active against Mycobacterium tuberculosis than pyrazinamide and also active against Mycobacterium avium and Mycobacterium intracellulare. Of the drugs synthesized, four drugs, namely, pyrazine
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8. Role of Acid pH and Deficient Efflux of Pyrazinoic Acid in Unique Susceptibility of Mycobacterium tuberculosis to Pyrazinamide
Pyrazinamide (PZA) is an important antituberculosis drug. Unlike most antibacterial agents, PZA, despite its remarkable in vivo activity, has no activity against Mycobacterium tuberculosis in vitro except at an acidic pH. M. tuberculosis is uniquely susceptible to PZA, but other mycobacteria as well as nonmycobacteria are intrinsically resistant. The role of
American Society for Microbiology.
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9. Does pyrazinoic acid as an active moiety of pyrazinamide have specific activity against Mycobacterium tuberculosis?
The commonly accepted hypothesis explaining the mechanism of action of pyrazinamide (PZA) is based on the assumption that PZA-susceptible Mycobacterium tuberculosis strains produce pyrazinamidase, which hydrolyzes PZA to the antibacterial moiety pyrazinoic acid (POA). It is not clear whether POA has specific antimicrobial activity or the inhibition of growth
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10. Photometabolism of Heterocyclic Aromatic Compounds by Rhodopseudomonas palustris OU 11
Rhodopseudomonas palustris OU 11 (ATCC 51186; DSM 7375) isolated from a pond of chemical industry effluent could anaerobically photometabolize heterocyclic aromatic compounds belonging to the pyridine and pyrazine groups only after a period of adaptation on pyrazinoic acid of 5 to 6 weeks. Growth on heterocyclic compounds was light dependent. The effects of
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11. Pyrazinoate Excretion in the Chimpanzee. RELATION TO URATE DISPOSITION AND THE ACTIONS OF URICOSURIC DRUGS
These experiments were designed to define the renal disposition of pyrazinoic acid in a nonhuman primate that is phylogenetically close to man and to relate this to the effects of pyrazinoate on urate excretion. The renal clearance of pyrazinoate was almost always greater than the simultaneous glomerular filtration rate at plasma concentrations ranging from
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12. Rapid Detection of Pyrazinamide-Resistant Mycobacterium tuberculosis by a PCR-Based In Vitro System
Pyrazinamide (PZA), an analog of nicotinamide, is a prodrug for tuberculosis which requires conversion to the bactericidal compound pyrazinoic acid by bacterial pyrazinamidase activity. Mutations leading to a loss of pyrazinamidase activity cause PZA resistance in Mycobacterium tuberculosis. Thus, the detection of pyrazinamidase activity makes the discrimina
American Society for Microbiology.