Zhang Zhenfa, Zhou Weicheng, Yu Aizhen
Biomolecular Structure Center, Department of Biochemistry, Box 357350, University of Washington, Seattle, WA 98195, USA.
Bioorg Med Chem Lett. 2004 Jan 19;14(2):393-5. doi: 10.1016/j.bmcl.2003.10.059.
A series of 7-(substituted)aminomethyl quinolones was synthesized and evaluated for antibacterial activity. Derivatives with (monoalkyl)aminomethyl substituent at C-7 displayed high in vitro activities comparable to Lomefloxacin against gram-negative organisms, whereas those bearing a [(substituted)phenyl]aminomethyl side chain at C-7 demonstrated good activities against gram-positive organisms as potent as Lomefloxacin and Vancomycin.
合成了一系列7 -（取代）氨甲基喹诺酮类化合物并评估其抗菌活性。在C-7位带有（单烷基）氨甲基取代基的衍生物在体外对革兰氏阴性菌显示出与洛美沙星相当的高活性，而在C-7位带有[（取代）苯基]氨甲基侧链的衍生物对革兰氏阳性菌表现出良好的活性，其效力与洛美沙星和万古霉素相当。
