Artico M, Mai A, Sbardella G, Massa S, Musiu C, Lostia S, Demontis F, La Colla P
Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, Italy.
Bioorg Med Chem Lett. 1999 Jun 21;9(12):1651-6. doi: 10.1016/s0960-894x(99)00251-6.
During search on quinolonecarboxylic acids we used a facile, convenient two- or three-step procedure to synthesize new quinolone analogs, bearing at the C-7 position alkylamino substituents, and at the C-6 position a fluorine or alternatively a nitro group. The new derivatives were tested against both Gram-positive and Gram-negative bacteria and against a number of different mycobacteria. In vitro assays showed 1-tert-butyl-7-tert-butylamino-6-nitro-1,4-dihydro-4-quinolone-3-carboxy lic acid to be a potent inhibitor of Streptococcus and Staphylococcus with potencies superior to those of ofloxacin and ciprofloxacin, used as reference drugs. Some 6-nitroquinolones were found to exert good inhibiting activities against Mycobacterium tuberculosis and various atypical mycobacteria, whereas the 6-fluoro counterparts showed poor or no activity against this bacterium.
在对喹诺酮羧酸进行研究的过程中，我们采用了简便易行的两步或三步程序来合成新的喹诺酮类似物，这些类似物在C-7位带有烷基氨基取代基，在C-6位带有氟原子或硝基。对这些新衍生物进行了针对革兰氏阳性菌和革兰氏阴性菌以及多种不同分枝杆菌的测试。体外试验表明，1-叔丁基-7-叔丁基氨基-6-硝基-1,4-二氢-4-喹诺酮-3-羧酸是链球菌和葡萄球菌的强效抑制剂，其效力优于用作参考药物的氧氟沙星和环丙沙星。发现一些6-硝基喹诺酮对结核分枝杆菌和各种非典型分枝杆菌具有良好的抑制活性，而6-氟类似物对该细菌的活性较差或无活性。
