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一些新型金刚烷衍生物的合成与抗菌活性评估

Synthesis and antimicrobial activity evaluation of some new adamantane derivatives.

作者信息

Caliş Unsal, Yarim Mine, Köksal Meriç, Ozalp Meral

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.

出版信息

Arzneimittelforschung. 2002;52(10):778-81.

Abstract

In this study, some new Schiff bases were synthesized as antimicrobial agents using benzaldehyde derivatives and 1- or 2-aminoadamantane. The structures of the synthesized compounds were confirmed by IR, 1H-NMR and elementary analysis. Antimicrobial activities of the synthesized compounds were tested against some bacteria and yeast-like fungi. The antimicrobial activity of the compounds was investigated by broth microdilution method using two Gram positive (Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212) and two Gram negative (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853) bacteria and yeast-like fungi (Candida albicans ATCC 90028, Candida krusei ATCC 6258, Candida parapsilosis ATCC 22019). The antifungal activity of 1-((2-chloro-3,4-dimethoxybenzylidene) amino(adamantane (compound 3) against C. krusei and C. parapsilosis (minimal inhibitory concentration 32 micrograms/ml) was higher than that of the other tested compounds.

摘要

在本研究中,使用苯甲醛衍生物和1-或2-氨基金刚烷合成了一些新型席夫碱作为抗菌剂。通过红外光谱、1H-核磁共振和元素分析确定了合成化合物的结构。测试了合成化合物对一些细菌和类酵母真菌的抗菌活性。采用肉汤微量稀释法,使用两种革兰氏阳性菌(金黄色葡萄球菌ATCC 25923、粪肠球菌ATCC 29212)、两种革兰氏阴性菌(大肠杆菌ATCC 25922、铜绿假单胞菌ATCC 27853)和类酵母真菌(白色念珠菌ATCC 90028、克柔念珠菌ATCC 6258、近平滑念珠菌ATCC 22019)研究了这些化合物的抗菌活性。1-((2-氯-3,4-二甲氧基苄基)亚氨基)金刚烷(化合物3)对克柔念珠菌和近平滑念珠菌的抗真菌活性(最低抑菌浓度为32微克/毫升)高于其他受试化合物。

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