Abstract
A series of alkyl α-[5-(5-nitro-2-thienyl)-1,3,4-thiadiazole-2-ylthio]acetic acid esters 6a– e were synthesized and evaluated for in vitro antituberculosis activity against Mycobacterium tuberculosis strain H 37Rv using the BACTEC 460 radiometric system and BACTEC 12B medium. The antituberculosis data indicated that methyl, propyl, buthyl and benzyl esters showed a significant in vitro antimycobacterium tuberculosis activity (MIC=0.39–0.78 μg/ml) and the ethyl analogue did not show a good activity (MIC>6.25 μg/ml, %inhibition=58). The most active compound of the series was n-propyl α-[5-(5-nitro-2-thienyl)-1,3,4-thiadiazole-2-ylthio]acetate ( 6c) with MIC value of 0.39 μg/ml.
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