Soliman R, Habib N S, Ashour F A, el-Taiebi M
Pharmaceutical Chemistry Department, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt.
Boll Chim Farm. 2001 May-Jun;140(3):140-8.
Four novel series of pyrazolylbenzimidazole derivatives have been prepared, namely 2-[(1-substituted phenyl-3,5-dimethyl-4-pyrazolyl)methyl]benzimidazole 5a-d 2-[(1-substituted phenyl-3-methyl-5-oxo-4,5-dihydro-4-pyrazolyl-4-yl)methyl]benzimidazoles 6a-d; 2-[(1-substituted phenyl-3,5-dioxopyrazolidin-4-yl)methyl]benzimidazoles 7a-d and 2-[(4-(1-phenyl-5-aryl-4,5-dihydro-3-pyrazolyl)phenylaminoacetyl]thio- methyl)-benzimidazoles 12a-e. The antimicrobial testing of the prepared compounds was performed using Escherichia Coli (NCTC 5933) as Gram-negative bacteria, Staphylococcus aureus (NCTC 4163) as gram-positive bacteria and Candida albicans (NCTC 5310) as yeast like fungi. The most potent compound was the pyrazolone 6a which exhibits interesting antibacterial activity against the gram-negative bacteria E. coli.
已经制备了四个新型的吡唑基苯并咪唑衍生物系列,即2-[(1-取代苯基-3,5-二甲基-4-吡唑基)甲基]苯并咪唑5a-d、2-[(1-取代苯基-3-甲基-5-氧代-4,5-二氢-4-吡唑基-4-基)甲基]苯并咪唑6a-d;2-[(1-取代苯基-3,5-二氧代吡唑烷-4-基)甲基]苯并咪唑7a-d和2-[(4-(1-苯基-5-芳基-4,5-二氢-3-吡唑基)苯基氨基乙酰基]硫代甲基)-苯并咪唑12a-e。使用大肠杆菌(NCTC 5933)作为革兰氏阴性菌、金黄色葡萄球菌(NCTC 4163)作为革兰氏阳性菌以及白色念珠菌(NCTC 5310)作为酵母样真菌对所制备的化合物进行抗菌测试。最有效的化合物是吡唑啉酮6a,它对革兰氏阴性菌大肠杆菌表现出有趣的抗菌活性。