新型铁载体共轭单氨基二醇的制备、革兰氏阴性抗菌活性及水解稳定性
Preparation, gram-negative antibacterial activity, and hydrolytic stability of novel siderophore-conjugated monocarbam diols.
作者信息
Flanagan Mark E, Brickner Steven J, Lall Manjinder, Casavant Jeffrey, Deschenes Laura, Finegan Steven M, George David M, Granskog Karl, Hardink Joel R, Huband Michael D, Hoang Thuy, Lamb Lucinda, Marra Andrea, Mitton-Fry Mark, Mueller John P, Mullins Lisa M, Noe Mark C, O'Donnell John P, Pattavina David, Penzien Joseph B, Schuff Brandon P, Sun Jianmin, Whipple David A, Young Jennifer, Gootz Thomas D
机构信息
Worldwide Medicinal Chemistry, Pharmaceutical Sciences, Antibacterials Research Unit, and Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development , Eastern Point Road, Groton, Connecticut 06340, United States.
SJ Brickner Consulting, LLC, Ledyard, Connecticut 06339, United States.
出版信息
ACS Med Chem Lett. 2011 Mar 2;2(5):385-90. doi: 10.1021/ml200012f. eCollection 2011 May 12.
Abstract
A novel series of monocarbam compounds exhibiting promising antibacterial activity against multidrug resistant Gram-negative microorganisms is reported, along with the synthesis of one such molecule MC-1 (1). Also reported are structure-activity relationships associated with the in vitro and in vivo efficacy of 1 and related analogues in addition to the hydrolytic stability of such compounds and possible implications thereof.
摘要
报道了一系列新型单氨基甲酸盐化合物，它们对多重耐药革兰氏阴性微生物具有有前景的抗菌活性，同时还报道了其中一种分子MC-1（1）的合成。除了此类化合物的水解稳定性及其可能的影响外，还报道了与1及相关类似物的体外和体内疗效相关的构效关系。
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