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

✍ Scribed by Phuong T. Le; Steven J. Brickner; Sarah K. Wade; Katherine Brighty; Rhonda Monahan; Gregory G. Stone; Dennis Girard; Steve Finegan; Joan Duignan; John Schafer; Meghan Maloney; Richard P. Zaniewski; Ann G. Connolly; Jennifer Liras; Jon Bordner; Ivan Samardjiev

• Publisher: Elsevier Science
• Year: 2011
• Tongue: English
• Weight: 863 KB
• Volume: 21
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.11.022

✦ Synopsis

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.