| abstract |
Novel compounds are disclosed having the structure of Formula I: wherein, n is an integer from 1 to 5; X is -CN, -F, -CI, -Br, -I, -N0 2 ; W is S, SO, S0 2 , O, NH, or NR 5 ; R 5 is alkyl, aralkyl, alkenyl, or alkynyl; Y is O, S; Z is NR 1 R 2 or heterocycloalkyl; R 1 , R 2 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups; R 3 and R 4 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups, and may together form a cyclic structure; and Ar is mono-, di-, or tri-substituted phenyl or heteroaryl, a pharmaceutically acceptable salts thereof. The compounds are potent bacterial efflux pump inhibitors (EPIs). Such compounds are useful to potentiate the antimicrobial activity of antimicrobial compounds such as beta-lactam antibiotics and quinolone antibiotics against Gram-negative bacteria. |