8-氮杂四环素类：一类新型四环素类抗菌药物的合成与评价。
8-Azatetracyclines: synthesis and evaluation of a novel class of tetracycline antibacterial agents.
机构信息
Tetraphase Pharmaceuticals, Inc, 480 Arsenal Street, Watertown, Massachusetts 02472, United States.
出版信息
J Med Chem. 2011 Mar 10;54(5):1511-28. doi: 10.1021/jm1015389. Epub 2011 Feb 8.
Abstract
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.
摘要
一系列新型全合成 8-氮杂四环素被制备并评估了其抗菌活性。鉴定出的化合物可克服外排（tet(K)) 和核糖体保护（tet(M)) 四环素耐药机制，对革兰氏阳性菌和革兰氏阴性菌均有活性。两种化合物在细菌感染的体内模型中表现出与市售四环素相当的疗效。
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