氟哌酸(NFLX.1)的发现不仅对于喹诺酮类抗菌剂本身,而且对口服抗感染药物,都开创了一个新的时代。它的出现极大地推动了喹诺酮类抗菌药物在临床上的应用。随着它的发现,又相继出现了许多包括其生物等配体(bioisostor)如氟啶酸(2)等的有关化合物,有不少已经上市(表一)。Koga等以前对结构如通式3的71个化合物进行了QSAR研究。从统计学角度得出 The discovery of norfloxacin (NFLX.1) opens a new era not only for quinolone antibacterial agents but also for oral anti-infectives. Its appearance has greatly promoted the clinical application of quinolone antibiotics. With its discovery, a number of related compounds have emerged, including bioisostats such as fiuidic acid (2), many of which are already on the market (Table 1). Koga et al. Conducted QSAR studies on 71 compounds of the general structure 3 previously. From a statistical point of view