OPPERMAN, TIMOTHY J.,NGUYEN, SON T.,KWASNY, STEVEN M.,DING, XIAOYUAN
申请号：
CA2910593
公开号：
CA2910593C
申请日:
2014.05.03
申请国别(地区):
CA
年份:
2018
代理人:
摘要：
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, -N02 W is S, SO, S02, O, NH, or NR5 R5 is alkyl, aralkyl, alkenyl, or alkynyl Y is O, S Z is NR1R2 or heterocycloalkyl R1, R2 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 R3 and R4 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.
