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2-氟苯基-4,6-二取代[1,3,5]三嗪的合成及抗菌活性。

Synthesis and antimicrobial activity of 2-fluorophenyl-4,6-disubstituted [1,3,5]triazines.

机构信息

ProMetic BioSciences Inc, 500 Boulevard Cartier Ouest, Laval, Québec, Canada.

出版信息

Bioorg Med Chem Lett. 2010 Feb 1;20(3):945-9. doi: 10.1016/j.bmcl.2009.12.063. Epub 2009 Dec 23.

Abstract

A series of 2-fluorophenyl-4,6-disubstituted [1,3,5]triazines (1) and (2) were synthesized and evaluated for their antimicrobial activity against three representative gram-positive bacteria and two fungi. The structure-activity relationship (SAR) demonstrates that the 3- or 4-fluorophenyl component attached directly to the triazine ring was essential for activity. Of these compounds, 14, 15, and 25 demonstrated significant activity against all selected organisms compared to control. These compounds were generally nontoxic and may prove useful as antimicrobial agents.

摘要

一系列 2-氟苯基-4,6-二取代[1,3,5]三嗪(1)和(2)被合成并评估了它们对三种代表性革兰氏阳性菌和两种真菌的抗菌活性。构效关系(SAR)表明,直接连接在三嗪环上的 3-或 4-氟苯基部分对于活性是必需的。在这些化合物中,14、15 和 25 与对照相比,对所有选定的生物体表现出显著的活性。这些化合物通常无毒性,可能证明作为抗菌剂是有用的。

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