Zhao Gaiying, Miller Marvin J, Franzblau Scott, Wan Baojie, Möllmann Ute
Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
Bioorg Med Chem Lett. 2006 Nov 1;16(21):5534-7. doi: 10.1016/j.bmcl.2006.08.045. Epub 2006 Aug 30.
The syntheses and anti-tuberculosis activity of quinolone-cephalosporin conjugates (1 and 2) are described. Both showed broad-spectrum antibacterial activity and significant anti-TB activity. The carbamate-linked quinolone-cephem 2 showed better antimycobacterial activity, including anti-TB activity, than the direct amine-linked quinolone-cephem 1, while quinolone-cephem 1 was slightly more effective against some Gram-negative bacterial strains.
描述了喹诺酮 - 头孢菌素缀合物（1和2）的合成及抗结核活性。两者均显示出广谱抗菌活性和显著的抗结核活性。与直接胺连接的喹诺酮 - 头孢烯1相比，氨基甲酸酯连接的喹诺酮 - 头孢烯2表现出更好的抗分枝杆菌活性，包括抗结核活性，而喹诺酮 - 头孢烯1对某些革兰氏阴性细菌菌株的效果略好。
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