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Indian J Exp Biol ; 2014 Nov; 52(11): 1062-1070
Article Dans Anglais | IMSEAR | ID: sea-153788

Résumé

Antimicrobial screening of several novel 4-thiazolidinones with benzothiazole moiety has been performed. These compounds were evaluated for antimicrobial activity against a panel of bacterial and fungal strains. The strains were treated with these benzothiazole derivatives at varying concentrations, and MIC’s were calculated. Structures of these compounds have been determined by spectroscopic studies viz., FT-IR, 1H NMR, 13C NMR and elemental analysis. Significant antimicrobial activity was observed for some members of the series, and compounds viz. 3-(4-(benzo[d]thiazol-2-yl) phenyl)-2-(4-methoxyphenyl)thiazolidin-4-one and 3-(4-(benzo[d]thiazol-2-yl)phenyl)-2-(4-hydroxy phenyl)thiazolidin-4-one were found to be the most active against E.coli and C.albicans with MIC values in the range of 15.6–125 μg/ml. Preliminary study of the structure–activity relationship revealed that electron donating groups associated with thiazolidine bearing benzothiazole rings had a great effect on the antimicrobial activity of these compounds and contributes positively for the action. DNA cleavage experiments gave valuable hints with supporting evidence for describing the mechanism of action and hence showed a good correlation between their calculated MIC’s and its lethality.


Sujets)
Antibactériens/synthèse chimique , Antibactériens/composition chimique , Antibactériens/pharmacologie , Antifongiques/synthèse chimique , Antifongiques/composition chimique , Antifongiques/pharmacologie , Benzothiazoles/synthèse chimique , Benzothiazoles/composition chimique , Benzothiazoles/pharmacologie , Candida/effets des médicaments et des substances chimiques , ADN bactérien/effets des médicaments et des substances chimiques , ADN circulaire/effets des médicaments et des substances chimiques , Tests d'agents antimicrobiens par diffusion à partir de disques , Évaluation préclinique de médicament , Électrophorèse sur gel d'agar , Piégeurs de radicaux libres/pharmacologie , Bactéries à Gram négatif/effets des médicaments et des substances chimiques , Bactéries à Gram positif/effets des médicaments et des substances chimiques , Tests de sensibilité microbienne , Structure moléculaire , Thiazolidines/synthèse chimique , Thiazolidines/composition chimique , Thiazolidines/pharmacologie
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