ACTA Pharmaceutica Sciencia 2011 , Vol 53 , Num 3
ANTIMICROBIAL AND CYTOTOXIC STUDIES OF NEW 2-SUBSTITUE-1H-BENZIMIDAZOLE DERIVATIVES
GÖRKEM SARIKAYA, AYŞE SELCEN ALPAN, HÜSEYİN TAŞLI, GÜLNUR SEVİN, CEREN GÖNEN KORKMAZ, HASAN SEMİH GÜNEŞ
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University, Bornova, Izmir, Turkey 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

Istanbul Medipol University