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

Autor: Le PT; Pfizer Worldwide Research & Development, La Jolla Laboratories, Pfizer Inc, La Jolla, CA 92121, United States. phuong.le@pfizer.com, Brickner SJ, Wade SK, Brighty K, Monahan R, Stone GG, Girard D, Finegan S, Duignan J, Schafer J, Maloney M, Zaniewski RP, Connolly AG, Liras J, Bordner J, Samardjiev I
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jan 01; Vol. 21 (1), pp. 276-9. Date of Electronic Publication: 2010 Nov 10.
DOI: 10.1016/j.bmcl.2010.11.022
Abstrakt: 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.
(Copyright © 2010 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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