8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents
8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents
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DOI：
10.1021/jm1015389
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发表时间：
2011-03-10
影响因子：
7.3
通讯作者：
Xiao, Xiao-Yi
中科院分区：
文献类型：
--
作者：
Clark, Roger B.;He, Minsheng;Xiao, Xiao-Yi
合成了一系列新的8-氮杂四环素类化合物，并对其抗菌活性进行了评价。鉴定了克服外排（泰特（K））和核糖体保护（泰特（M））四环素抗性机制的化合物，并对革兰氏阳性和革兰氏阴性微生物具有活性。鉴定了两种化合物，其在细菌感染的体内模型中表现出与市售四环素相当的功效。
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.