Synthesis and antimicrobial activity of 4-trifluoromethylpyridine nucleosides

Abstract

4-Trifluoromethylpyridine derivatives 4-8 represent good candidates for the discovery of new antibacterial agents. Fluorinated pyridine nucleosides 4-7 and non-nucleoside analogues 8a,b were synthesized and evaluated for their antibacterial activities against Staphylococcus aureus, Bacillus infantis, Escherichia coli and Stenotrophomonas maltophilia. The minimum inhibitory concentrations (MICs) of the new nucleosides 4-7 range from 1.3 to 4.9 μg/mL and MICs of fluoroaryl derivatives 8a,b are in the range of 1.8-5.5 μg/mL. Activity of amoxicillin, the reference drug, is 1.0-2.0 μg/mL under similar conditions.