Küçükbay H, Cetinkaya E, Durmaz R
Department of Chemistry, Faculty of Science and Literature, Inönü University, Malatya, Turkey.
Arzneimittelforschung. 1995 Dec;45(12):1331-4.
New benzimidazole, benzothiazole and imidazole derivatives were synthesized by reacting electron-rich olefins (5, 23 and 29) with appropriate reagents. The compounds synthesized were identified by 1H, 13C-NMR, FT-IR and mass spectroscopic techniques and micro analysis. All new and related compounds were evaluated for their in vitro antimicrobial activity against different bacteria. The compounds 17, 18, 19, 20, 21, 22 and 24 were found very effective to inhibit the growth of Enterococcus faecalis (ATCC 29212) and Staphylococcus aureus (ATCC 29213) at minimum inhibitory concentrations (MICs) of 25, 25, 12.5, 50, 25, 50 and 50 micrograms/ml, respectively. The compounds 4, 10a, 10c, 16, 25, 26 and 31 were significantly effective against Enterococcus faecalis (ATCC 29212) and Staphylococcus aureus (ATCC 29213) with MIC values of 100-200 micrograms/ml. None of the compounds proved to be effective against Escherichia coli (ATCC 25922) and Pseudomonas aeruginosa (ATCC 27853) in the concentrations studied.
通过使富电子烯烃（5、23和29）与适当的试剂反应，合成了新的苯并咪唑、苯并噻唑和咪唑衍生物。通过1H、13C-NMR、傅里叶变换红外光谱（FT-IR）和质谱技术以及微量分析对合成的化合物进行了鉴定。对所有新的及相关化合物针对不同细菌的体外抗菌活性进行了评估。发现化合物17、18、19、20、21、22和24在最低抑菌浓度（MIC）分别为25、25、12.5、50、25、50和50微克/毫升时，对粪肠球菌（ATCC 29212）和金黄色葡萄球菌（ATCC 29213）的生长具有非常有效的抑制作用。化合物4、10a、10c、16、25、26和31对粪肠球菌（ATCC 29212）和金黄色葡萄球菌（ATCC 29213）具有显著效果，MIC值为100 - 200微克/毫升。在所研究的浓度下，没有一种化合物对大肠杆菌（ATCC 25922）和铜绿假单胞菌（ATCC 27853）有效。
