Göker H, Tunçbilek M, Ayhan G, Altanlar N
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Turkey.
Farmaco. 1998 Jun 30;53(6):415-20. doi: 10.1016/s0014-827x(98)00045-7.
A series of 1,2-disubstituted benzimidazole-5(6)-carboxamides was prepared and evaluated in vitro for antimicrobial activity against Staphyloccus aureus, Escherichia coli and Candida albicans. The precursor benzimidazolecarboxylic acids 4a-c and 9a-c were prepared via oxidative condensation of diaminobenzoic acids with aldehydes and via several steps over the 2(1H)-benzimidazolones, respectively. All acids were converted to their acyl chlorides with SOCl2, then amidified with several N,N'-dialkylaminoethyl derivatives. Compounds 8a-c, 20 and 22 exhibited the best activity.
制备了一系列1,2-二取代苯并咪唑-5(6)-甲酰胺，并对其进行体外抗金黄色葡萄球菌、大肠杆菌和白色念珠菌的抗菌活性评估。前体苯并咪唑羧酸4a-c和9a-c分别通过二氨基苯甲酸与醛的氧化缩合以及经过几步从2(1H)-苯并咪唑酮制备得到。所有酸都用亚硫酰氯转化为它们的酰氯，然后与几种N,N'-二烷基氨基乙基衍生物进行酰胺化反应。化合物8a-c、20和22表现出最佳活性。
