Fluorocyclines. 1. 7-Fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: A Potent, Broad Spectrum Antibacterial Agent

详细信息    查看全文

• 作者：Xiao-Yi Xiao ; Diana K. Hunt ; Jingye Zhou ; Roger B. Clark ; Nick Dunwoody ; Corey Fyfe ; Trudy H. Grossman ; William J. O鈥橞rien ; Louis Plamondon ; Magnus R枚nn ; Cuixiang Sun ; Wu-Yan Zhang ; Joyce A. Sutcliffe
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：January 26, 2012
• 年：2012
• 卷：55
• 期：2
• 页码：597-605
• 全文大小：378K
• 年卷期：v.55,no.2(January 26, 2012)
• ISSN：1520-4804

文摘

This and the accompanying report (DOI: 10.1021/jm201467r) describe the design, synthesis, and evaluation of a new generation of tetracycline antibacterial agents, 7-fluoro-9-substituted-6-demethyl-6-deoxytetracyclines (鈥渇luorocyclines鈥?, accessible through a recently developed total synthesis approach. These fluorocyclines possess potent antibacterial activities against multidrug resistant (MDR) Gram-positive and Gram-negative pathogens. One of the fluorocyclines, 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline (17j, also known as TP-434, 50th Interscience Conference on Antimicrobial Agents and Chemotherapy Conference, Boston, MA, September 12鈥?5, 2010, poster F1鈥?157), is currently undergoing phase 2 clinical trials in patients with complicated intra-abdominal infections (cIAI).