Synthesis and Antimycobacterial Activity of 2-aryl-3-(arylmethyl)-1,3-thiazolidin-4-ones

Authors: Gomes, C.R.B. ; Da Silva, M.M.; Facchinetti, V.; De Souza, M.V.N.; Vellasco, Jr., W.T.; Lourenço, M.C.S.; Cunico, W.


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, DrugsDocument Type: Research ArticleDOI: http://dx.doi.org/10.2174/157018010791163451Publication date: 1 de Janeiro de 2010

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