SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF PYRIMIDINOPHANES CONTAINING A URACIL MOIETY AND A BRIDGING SULFUR ATOM

被引：9

作者：

Nikolaev, A. E. ^{[1
]}

Semenov, V. E. ^{[1
]}

Voloshina, A. D. ^{[1
]}

Kulik, N. V. ^{[1
]}

Reznik, V. S. ^{[1
]}

机构：

[1] Russian Acad Sci, Kazan Sci Ctr, AE Arbuzov Organ & Phys Chem Inst, Kazan, Russia

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2010年 / 44卷 / 03期

基金：

俄罗斯基础研究基金会;

关键词：

Pyrimidinophanes; uracils; sulfonium group; antibacterial activity; DERIVATIVES; ANTIBACTERIAL; POLYMERS;

D O I：

10.1007/s11094-010-0414-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pyrimidinophanes containing one 5(6)-alkylsubstituted uracil moiety and a 10- or 12-methylene bridge including a sulfur atom were synthesized. The bridging S atoms of the macrocycles were converted to sulfonium groups by interaction with para-toluenesulfonate methyl or nonyl esters. The resulting amphiphilic pyrimidinophanes were tested for bacteriostatic and fungistatic activity against Gram-positive and Gram-negative bacteria and fungi. Amphiphilic pyrimidinophanes with 5-decyl-6-methyluracil moieties had high levels of bacteriostatic activity against Gram-positive bacteria. The minimum inhibitory concentration of the macrocycle containing a methyl group in the sulfonium grouping against Staphylococcus aureus was 0.75 mu g/ml. These data are of value in seeking new highly effective antimicrobial agents.

引用

页码：130 / 133

页数：4

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