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ACTA Pharmaceutica Sciencia
2011 , Vol 53 , Num 3
ANTIMICROBIAL AND CYTOTOXIC STUDIES OF NEW 2-SUBSTITUE-1H-BENZIMIDAZOLE DERIVATIVES
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University, Bornova, Izmir, Turkey
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We synthesized a series of 2-substituted-1H-benzimidazole derivatives (1-9) of which six of them were original and elucidated their structures by spectral analyses. We also evaluated the in-vitro antimicrobial activities of the synthesized compounds and detected potent inhibitory action in some of the compounds. Moreover, 2-(1H-benzimidazole-2-yl)phenol intermediates, bearing o-hydroxyphenyl substituent on 1H-benzimidazole ring possess equal or similar results compared to the standard compound, Ceftazidime. The synthesized compounds didn’t show any significant antifungal activity on Candida albicans. All nine 1H-benzimidazole derivatives were tested for their cytotoxicity through WST-1 colorimetric assay-based in vitro tests on the mammalian LNCaP cell line. Compounds 7 and 8 were found to have IC50 values of 0,09 ± 0,01 μM and 0,03 ± 0,02 μM, respectively. It is noteworthy that the values obtained with these two compounds were highly comparable to that of Doxorubicine 0,053 ± 0,003 μM, the reference drug used in our study.
Keywords :
ANTIBACTERIAL, ANTIFUNGAL, CYTOTOXICITY, BENZIMIDAZOLES, SYNTHESIS