Abstract
Fifteen new heterocyclic thiazolidinones have been synthesized from one-pot reactions of piperonylamine, arenealdehydes and mercaptoacetic acid. These compounds plus ten 2-aryl-3-(benzyl)-1,3-thiazolidin-4-ones which had been previously synthesized, were evaluated as antibacterial agents against Mycobacterium tuberculosis H37Rv using the Alamar Blue susceptibility test and their activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. Six of the series exhibited modest activity when compared to the first line drugs such as isoniazid (INH) and rifampicin (RIP). Therefore this class of compounds could be a good starting point to develop new lead compounds in the treatment of multi-drug resistant tuberculosis.
Keywords: Tuberculosis, Thiazolidinones, Drugs
Letters in Drug Design & Discovery
Title: Synthesis and Antimycobacterial Activity of 2-aryl-3-(arylmethyl)-1,3-thiazolidin-4-ones
Volume: 7 Issue: 5
Author(s): Claudia R.B. Gomes, Marcele Moreth, Victor Facchinetti, Marcus V.N. de Souza, Walcimar T. Vellasco Junior, Maria Cristina da Silva Lourenco and Wilson Cunico
Affiliation:
Keywords: Tuberculosis, Thiazolidinones, Drugs
Abstract: Fifteen new heterocyclic thiazolidinones have been synthesized from one-pot reactions of piperonylamine, arenealdehydes and mercaptoacetic acid. These compounds plus ten 2-aryl-3-(benzyl)-1,3-thiazolidin-4-ones which had been previously synthesized, were evaluated as antibacterial agents against Mycobacterium tuberculosis H37Rv using the Alamar Blue susceptibility test and their activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. Six of the series exhibited modest activity when compared to the first line drugs such as isoniazid (INH) and rifampicin (RIP). Therefore this class of compounds could be a good starting point to develop new lead compounds in the treatment of multi-drug resistant tuberculosis.
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R.B. Gomes Claudia, Moreth Marcele, Facchinetti Victor, V.N. de Souza Marcus, T. Vellasco Junior Walcimar, Cristina da Silva Lourenco Maria and Cunico Wilson, Synthesis and Antimycobacterial Activity of 2-aryl-3-(arylmethyl)-1,3-thiazolidin-4-ones, Letters in Drug Design & Discovery 2010; 7 (5) . https://dx.doi.org/10.2174/157018010791163451
DOI https://dx.doi.org/10.2174/157018010791163451 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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