The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: A novel potent antibacterial analog derived from hygromycin A

SAR studies and optimization of various modified Hygromycin A fluoroalkyl ethers, which led to the discovery of the highly potent 4′-(2-cyclopropyl-2-fluoroethyl ether) antibacterial CE-156811 (1) derived from truncation of the ribose ring and difluorination of the phenyl found in Hygromycin A, are discussed.