一些源自6-酰基-3-(3,5-二甲基哌啶甲基)-2(3H)-苯并恶唑酮的新型曼尼希碱的合成及其生物活性。
Synthesis of some new Mannich bases derived from 6-acyl-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benzoxazolones+ ++ and their biological activities.
作者信息
Erol D D, Rosen A, Erdogan H, Yulug N
机构信息
University of Hacettepe, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.
出版信息
Arzneimittelforschung. 1989 Aug;39(8):851-3.
A number of 6-acyl-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benzoxazolones have been synthesized by Mannich reaction and their antibacterial and antifungal activities have been tested. Their chemical structures have been proved by means of their IR, NMR, mass spectroscopic data and by elementary analysis. Investigation of antimicrobial activity of compounds was done by tube dilution and paper disc techniques using bacteria (Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Staphylococcus faecalis RSKK 10541) and yeast-like fungi (Candida parapsilosis, Candida albicans, Candida pseudotropicalis, Candida stellatoidea). Among the compounds tested 6-(2-chlorobenzoyl)-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benz oxazolone (Compound 2) and 6-(3-chlorobenzoyl)-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benz oxazolone (Compound 3) showed the most favorable activity.
通过曼尼希反应合成了一系列6-酰基-3-(3,5-二甲基哌啶甲基)-2(3H)-苯并恶唑酮，并测试了它们的抗菌和抗真菌活性。通过红外光谱、核磁共振、质谱数据和元素分析证实了它们的化学结构。采用试管稀释法和纸片法，以细菌（大肠杆菌ATCC 25922、金黄色葡萄球菌ATCC 25923、铜绿假单胞菌ATCC 27853、粪肠球菌RSKK 10541）和类酵母真菌（近平滑念珠菌、白色念珠菌、伪热带念珠菌、星状念珠菌）为受试对象，对化合物的抗菌活性进行了研究。在所测试的化合物中，6-(2-氯苯甲酰基)-3-(3,5-二甲基哌啶甲基)-2(3H)-苯并恶唑酮（化合物2）和6-(3-氯苯甲酰基)-3-(3,5-二甲基哌啶甲基)-2(3H)-苯并恶唑酮（化合物3）表现出最良好的活性。
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