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图1中1和2为代表的两类氟代喹诺酮抗感染药物,它们已引起世界各实验室和临床的极大兴趣。最早的药物是氟啶酸(1a),氟哌酸(1b)、甲氟哌酸(1c)和氟嗪酸(2a),这些药物在R,位上都有哌嗪基,R_1位有二原子基团,对R_1取代基最成功的结构改造是用卤代苯基(22氟哌酸1d)和环丙基(丙氟哌酸1e)。在对4-喹诺酮7位和8位(R7和X)构效关系研究已证明,氟基取代的吡咯烷是哌嗪侧链有效的模拟基团,它们对革蓝氏阳性菌
Two classes of fluoroquinolone anti-infectives, represented by 1 and 2 in Figure 1, have drawn great interest from laboratories and clinics around the world. The earliest drugs were fiuidinic acid (1a), norfloxacin (1b), cofloxacin (1c) and triflusal (2a). These drugs all have piperazinyl groups at the R, The most successful structural modification of the R <1> substituent by the atomic group is the use of a halophenyl group (22 norfloxacin 1d) and cyclopropyl (prenyl norfloxene). Studies on the structure-activity relationships of the 7-position and the 8-position of 4-quinolones (R7 and X) have shown that fluoro-substituted pyrrolidines are potent mimic groups in the piperazine side chain and are effective against Gram-positive bacteria