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氮烯硫化物--CXVIII. 新型 1-甲基-3-硫代-4-氨基喹啉鎓盐的抗菌活性。

Azinyl sulfides--CXVIII. Antimicrobial activity of novel 1-methyl-3-thio-4-aminoquinolinium salts.

机构信息

Department of Organic Chemistry, The Medical University of Silesia, 41-200, Sosnowiec, Poland.

出版信息

Folia Microbiol (Praha). 2010 Jan;55(1):3-9. doi: 10.1007/s12223-010-0001-1. Epub 2010 Mar 25.

Abstract

Synthesis and antimicrobial activity of novel 1-methyl-3-alkylthio-4-aminoquinolinium salts 2 and 1-methyl-3-acylthio-4-aminoquinolinium salts 4 are described. Compounds 2 were obtained by reacting 1-methyl-3,4-(dimethylthio)quinolinium chloride 1 with amines and by reacting 1-methyl-4-aminoquinolinium-3-thiolates 3 with alkylating agents. Compounds 4 were obtained by the reaction of 1-methyl-4-aminoquinolinium-3-thiolates 3 with acylating agents. Antimicrobial activity of compounds 2 and 4 was determined using G+ (Staphylococcus aureus, Enterococcus faecalis) and G(-) (Escherichia coli, Pseudomonas aeruginosa) strains as well as Candida albicans yeast. The compounds show greatest activity against S. aureus whereas the lowest against P. aeruginosa.

摘要

新型 1-甲基-3-烷基硫代-4-氨基喹啉鎓盐 2 和 1-甲基-3-酰基硫代-4-氨基喹啉鎓盐 4 的合成及抗菌活性的研究。化合物 2 通过 1-甲基-3,4-(二甲基硫代)喹啉鎓氯化物 1 与胺反应,以及 1-甲基-4-氨基喹啉-3-硫醇盐 3 与烷基化试剂反应得到。化合物 4 通过 1-甲基-4-氨基喹啉-3-硫醇盐 3 与酰化试剂反应得到。采用 G+(金黄色葡萄球菌、粪肠球菌)和 G-(大肠杆菌、铜绿假单胞菌)菌株以及白色念珠菌酵母来测定化合物 2 和 4 的抗菌活性。这些化合物对金黄色葡萄球菌的活性最大,而对铜绿假单胞菌的活性最小。

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