Küçükbay Hasan, Durmaz Riza, Orhan Ersin, Günal Selami
Department of Chemistry, Faculty of Arts and Sciences, Inönü University, 44069 Malatya, Turkey.
Farmaco. 2003 Jun;58(6):431-7. doi: 10.1016/S0014-827X(03)00068-5.
New benzimidazole derivatives were synthesised by electron-rich olefines (7, 8 and 9) with appropriate reagents. The compounds synthesised were identified by 1H NMR, 13C NMR, FT-IR spectroscopic techniques and elemental analysis. All compounds studied in this work were screened for their in vitro antimicrobial activities against the standard strains: Enterococcus faecalis (ATCC 29212), Staphylococcus aureus (ATCC 29213), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and the yeasts Candida albicans and Candida tropicalis. Eleven of the compounds inhibited the growth of gram-positive bacteria (E. faecalis and S. aureus) at MIC values between 50 and 400 microg/ml. None of the compounds exhibit antimicrobial activity against Gram-negative bacteria (E. coli and P. Aeruginosa) at the concentrations studied (6.25-800 microg/ml). Nine of the tested compounds showed an antifungal activity with a range of the MICs between 50 and 400 microg/ml.
通过富电子烯烃(7、8和9)与适当的试剂合成了新的苯并咪唑衍生物。通过1H NMR、13C NMR、FT-IR光谱技术和元素分析对合成的化合物进行了鉴定。对本研究中所有化合物针对标准菌株粪肠球菌(ATCC 29212)、金黄色葡萄球菌(ATCC 29213)、大肠杆菌(ATCC 25922)、铜绿假单胞菌(ATCC 27853)以及白色念珠菌和热带念珠菌进行了体外抗菌活性筛选。其中11种化合物在50至400微克/毫升的最低抑菌浓度(MIC)值下抑制革兰氏阳性菌(粪肠球菌和金黄色葡萄球菌)的生长。在所研究的浓度(6.25至800微克/毫升)下,没有一种化合物对革兰氏阴性菌(大肠杆菌和铜绿假单胞菌)表现出抗菌活性。9种受试化合物表现出抗真菌活性,最低抑菌浓度范围在50至400微克/毫升之间。