“甘氨酰环素”。3. 9-氨基多西环素羧酰胺。
"Glycylcyclines". 3. 9-Aminodoxycyclinecarboxamides.
作者信息
Barden T C, Buckwalter B L, Testa R T, Petersen P J, Lee V J
机构信息
Agricultural Research Division, American Cyanamid Company, Princeton, New Jersey 08543-0400.
出版信息
J Med Chem. 1994 Sep 30;37(20):3205-11. doi: 10.1021/jm00046a003.
A series of 9-(acylamino)doxycycline derivatives has been prepared. These analogs exhibit good activity against both tetracycline sensitive and tetracycline resistant Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria that are encoded with the efflux and ribosomal resistance gene factors. N,N-Dialkylglycylamido derivatives possessed the highest activity. Replacement of glycine moiety with other amino acids did not further enhance the activity.
已经制备了一系列9-（酰基氨基）多西环素衍生物。这些类似物对携带外排和核糖体抗性基因因子的四环素敏感和四环素抗性革兰氏阳性菌（金黄色葡萄球菌）和革兰氏阴性菌（大肠杆菌）均表现出良好的活性。N，N-二烷基甘氨酰胺基衍生物具有最高的活性。用其他氨基酸取代甘氨酸部分并没有进一步提高活性。
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