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  • Antituberculosis agents VIII
  • Add time:07/15/2019         Source:sciencedirect.com

    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 H37Rv 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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