Synthesis and evaluation of a pyrazinoic acid prodrug in Mycobacterium tuberculosis
| Autor: | Clarice Queico Fujimura Leite, Veni Maria Andres Felli, João Paulo-dos Santos Fernandes, Fernando Rogério Pavan |
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| Přispěvatelé: | Universidade de São Paulo (USP), Universidade Estadual Paulista (Unesp) |
| Jazyk: | angličtina |
| Předmět: |
Pharmacology
Activity profile MYCOBACTERIUM TUBERCULOSIS Pyrazinoic acid Tuberculosis Antimycobacterial agent biology business.industry Short Communication Pharmaceutical Science Prodrug biology.organism_classification medicine.disease Microbiology Mycobacterium tuberculosis chemistry.chemical_compound chemistry Pyrazinoate Medicine Tuberculostatic Ester synthesis business |
| Zdroj: | Web of Science Repositório Institucional da UNESP Universidade Estadual Paulista (UNESP) instacron:UNESP Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual) Universidade de São Paulo (USP) instacron:USP |
| ISSN: | 1319-0164 |
| DOI: | 10.1016/j.jsps.2013.12.005 |
| Popis: | Made available in DSpace on 2015-03-18T15:53:38Z (GMT). No. of bitstreams: 0 Previous issue date: 2014-09-01Bitstream added on 2015-03-18T16:29:16Z : No. of bitstreams: 1 WOS000341120900013.pdf: 475906 bytes, checksum: 9624095386cff64abf26bfd60673becd (MD5) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) PROPE Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Tuberculosis (TB) is a disease caused mainly by infection of Mycobacterium tuberculosis affecting more than ten million people around the world. Despite TB can be treated, the rise of MDR-TB and XDR-TB cases put the disease in a worrying status. As pyrazinamide-resistant strains exhibit low or none pyrazinamidase activity, it is proposed that the active form of pyrazinamide (PZA) is pyrazinoic acid (POA), although this acid has poor penetration in mycobacteria. In this work, we present a convenient one-pot synthesis of 2-chloroethyl pyrazinoate, and its activity in M. tuberculosis H(37)Rv (ATCC27294) in MIC assay using the MABA technique. The obtained MIC of the compound was 3.96 g/mL, and discussion about the activity profile of some previously evaluated pyrazinoates is also performed. (C) 2013 King Saud University. Production and hosting by Elsevier B.V. All rights reserved. Fed Univ Sao Paulo UNIFESP, Inst Environm Chem & Pharmaceut Sci, Sao Paulo, Brazil State Univ Sao Paulo UNESP, Fac Pharmaceut Sci, Dept Biol Sci, Sao Paulo, Brazil Univ Sao Paulo, Fac Pharmaceut Sci, Dept Pharm, BR-05508 Sao Paulo, Brazil State Univ Sao Paulo UNESP, Fac Pharmaceut Sci, Dept Biol Sci, Sao Paulo, Brazil |
| Databáze: | OpenAIRE |
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