alexa Abstract | Green synthesis and preliminary pharmacological evaluation of three-substituted thiazide derivatives as antibacterial agents

Journal of Chemical and Pharmaceutical Research
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2-Aminothiazole has great biological and medicinal interest. Some of the marketed drugs also possessed this heterocyclic moiety. This manuscript reports the synthesis of a series of 2-Aminothiazole derivatives. The reaction between secondary amines, benzoyl isothiocyanate, and dialkyl acetylene dicarboxylates(=dialkyl but-2-ynedioates) in the presence of silica gel (SiO2), led to alkyl 2-(dialkylamino)-4-phenylthiazole-5-carboxylates (6a-6l) in fairly high yields. All title compounds were characterized by IR, NMR and Mass spectroscopy. The antimicrobial activity of the compounds were evaluated against the following microorganisms: Staphylococcus epidermidis ATCC.14990, Bacillus subtilis ATCC.12711, Pseudomonas aeruginosa ATCC 27853Staphylococcus aureus ATCC 25923, Acinetobacter calcoaceticus ATCC 23055, and Escherichia coli ATCC 25922. The broth macrodilution method was used for determination of the minimum inhibitory concentration (MIC) during preliminary evaluation of antibacterial activity. The compounds yielded MIC values in the range of 7to3.9μg/mL for Staphylococcus aureus, 500 to 7μg/mL for Staphylococcus epidermidis, 62.5 to 0.097, for Bacillus subtilis, 500 to125 μg/mL, for Pseudomonas aeruginosa and 500 to 250forAcinetobactercalcoaceticus.The best MIC value with compounds 6a-6l was obtained for compounds 6e, 6f, 6g and 6h against Staphylococcus aureus and Bacillus subtilis.

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Author(s): Maryam Kouhkan Nima Hussein Jazani Ali Souldozi Minoo Zardashti and Narges Darabi


Antimicrobial activity, Minimum Inhibitory Concentration, Aminotiazol, antibacterial activity, In vitro, pharmacological evaluation

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