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

被引：58

作者：

Saleh, Mona ^{[1
]}

Abbott, Shaun ^{[1
]}

Perron, Valerie ^{[1
]}

Lauzon, Caroline ^{[1
]}

Penney, Christopher ^{[1
]}

Zacharie, Boulos ^{[1
]}

机构：

[1] ProMet BioSci Inc, Laval, PQ H7V 5B7, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期

关键词：

Fluorophenyl triazines; Rigid alkyl amines; Drug resistance; Antimicrobial activity; ANTIFUNGAL AGENTS; AMPHOTERICIN-B; DERIVATIVES; RESISTANCE; TRIAZINES; PRODUCTS;

D O I：

10.1016/j.bmcl.2009.12.063

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2009 Elsevier Ltd. All rights reserved.

引用

页码：945 / 949

页数：5

共 21 条

[1] Design and synthesis of a series of melamine-based nitroheterocycles with activity against trypanosomatid parasites [J].