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

…, S Finegan, J Duignan, J Schafer, M Maloney…

Index: Le, Phuong T.; Brickner, Steven J.; Wade, Sarah K.; Brighty, Katherine; Monahan, Rhonda; Stone, Gregory G.; Girard, Dennis; Finegan, Steve; Duignan, Joan; Schafer, John; Maloney, Meghan; Zaniewski, Richard P.; Connolly, Ann G.; Liras, Jennifer; Bordner, Jon; Samardjiev, Ivan Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 276 - 279

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Abstract

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.