A study on the genotoxic activities of some new benzoxazoles |
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Authors: | Emine Oksuzoglu Ozlem Temiz-Arpaci Betul Tekiner-Gulbas Hatice Eroglu Gulseren Sen Sabiha Alper Ilkay Yildiz Nuran Diril Esin Aki-Sener Ismail Yalcin |
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Institution: | (1) Molecular Biology Department, Faculty of Science, Hacettepe University, Beytepe, 06532, Ankara, Turkey;(2) Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ankara University, Tandogan, TR-06100, Ankara, Turkey |
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Abstract: | The Bacillus subtilis
rec assay has been specially developed to detect DNA-damaging potential in chemicals, with the rationale based on the relative
difference of survival of a DNA repair combination proficient strains and its deficient strain, which is interpreted as genotoxicity.
The genotoxic activities of newly (1–6) and previously (7–18) synthesized various benzoxazoles and benzimidazoles were analyzed via the B. subtilis
rec assay. Newly obtained benzoxazole and benzimidazole derivatives (1–6) were synthesized in the presence of polyphosphoric acid (PPA) and 6 N HCl, respectively to detect their DNA-damaging activities.
Among the tested compounds, 6-methyl-2-(o-chlorophenyl)benzoxazole (9), 5-amino-2-(p-methylbenzyl)benzoxazole (4), 5-(p-fluorobenzamido)-2-phenylbenzoxazole (13), and 2-(p-methylaminophenyl)benzoxazole (18) showed genotoxic activities having Rec50 values of 1.85, 1.74, 1.60, and 1.50 or S-probit values of 0.534, 0.482, 0.460, and 0.357, respectively. On the other hand,
2-(p-bromobenzyl)-5-methylbenzimidazole (6) and 2-benzyl-5-(p-fluorophenylacetamido)-benzoxazole (15) were exhibited a reverse effect that displayed a bacterial growth in the rec
- strains while there was no any bacterial growth in rec
+ strains at the same concentration. |
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Keywords: | Bacillus subtilis rec assay Benzimidazoles Benzoxazoles DNA-damaging activity Genotoxic activity |
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