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

Bioorganic & medicinal chemistry letters 2009 Dec 23; In press

Link to PubMed abstract

Saleh M, Abbott S, Perron V, Lauzon C, Penney C, Zacharie B

ProMetic BioSciences Inc., 500 Boulevard Cartier Ouest, Bureau 150, Laval, Québec, Canada H7V 5B7.

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.

Keywords: antimicrobial