Cationic cholic acid derivatives displayed potent and broad-spectrum activi
ty against multidrug-resistant Gram-negative and -positive bacteria, Specif
ic examples were effective permeabilizers of the outer membranes of many st
rains of multidrug-resistant Gram-negative bacteria and sensitized these to
hydrophobic antibiotics, We also prepared a new cholic acid derivative wit
h improved apparent selectivity for prokaryote membranes.