发现并研究结构-活性关系，得到 CE-156811，一种二氟苯基环丙基氟醚：一种新型的来源于潮霉素 A 的强效抗菌类似物。
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
机构信息
Pfizer Worldwide Research & Development, La Jolla Laboratories, Pfizer Inc, La Jolla, CA 92121, United States.
出版信息
Bioorg Med Chem Lett. 2011 Jan 1;21(1):276-9. doi: 10.1016/j.bmcl.2010.11.022. Epub 2010 Nov 10.
PMID:21115249
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.
摘要
SAR 研究和各种修饰的 Hygromycin A 氟烷基醚的优化，导致了从 Hygromycin A 中发现的核糖环截断和苯环的二氟化的高度有效的 4'-(2-环丙基-2-氟乙基醚)抗菌 CE-156811（1），讨论了。
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