8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents

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• 作者：Roger B. Clark ; Minsheng He ; Corey Fyfe ; Denene Lofland ; William J. O鈥橞rien ; Louis Plamondon ; Joyce A. Sutcliffe ; Xiao-Yi Xiao
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：March 10, 2011
• 年：2011
• 卷：54
• 期：5
• 页码：1511-1528
• 全文大小：1245K
• 年卷期：v.54,no.5(March 10, 2011)
• ISSN：1520-4804

文摘

A novel series of fully synthetic 8-azatetracyclines was prepared and evaluated for antibacterial activity. Compounds were identified that overcome both efflux (tet(K)) and ribosomal protection (tet(M)) tetracycline resistance mechanisms and are active against Gram-positive and Gram-negative organisms. Two compounds were identified that exhibit comparable efficacy to marketed tetracyclines in in vivo models of bacterial infection.