School of Pharmaceutical Science, Sun Yat-Sen University, Guangzhou 510006, China.
Bioorg Med Chem Lett. 2010 May 1;20(9):2859-63. doi: 10.1016/j.bmcl.2010.03.044. Epub 2010 Mar 12.
A series of 4-substituted 4-(1H-1,2,3-triazol-1-yl)piperidine building blocks was synthesized and introduced to the C7 position of the quinolone core, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid, to afford the corresponding fluoroquinolones in 40-83% yield. The antibacterial activity of these new fluoroquinolones was evaluated using a standard broth microdilution technique. Among them, the quinolone 1-cyclopropyl-6-fluoro-7-(4-(4-formyl-1H-1,2,3-triazol-1-yl)piperidin-1-yl)-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid (34.15) exhibited comparable antibacterial activity against quinolone-susceptible and multidrug-resistant strains, especially to Staphylococcus aureus and Staphylococcus epidermidis, in comparison with ciprofloxacin and vancomycin.
一系列 4-取代的 4-(1H-1,2,3-三唑-1-基)哌啶砌块被合成并引入到喹诺酮核心的 C7 位置，即 7-氯-1-环丙基-6-氟-4-氧代-1,4-二氢-1,8-萘啶-3-羧酸，以 40-83%的收率得到相应的氟喹诺酮。这些新的氟喹诺酮的抗菌活性通过标准肉汤微量稀释技术进行评估。其中，喹诺酮 1-环丙基-6-氟-7-(4-(4-甲酰基-1H-1,2,3-三唑-1-基)哌啶-1-基)-4-氧代-1,4-二氢-1,8-萘啶-3-羧酸（34.15）对喹诺酮敏感和多药耐药菌株的抗菌活性与环丙沙星和万古霉素相当，特别是对金黄色葡萄球菌和表皮葡萄球菌。
