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近年来,氟喹诺酮类抗菌药物的研究发展十分迅速。早期的构效关系研究表明,N-1位取代基对抗菌活性至关重要,如在N-1位引入氨基,可增加亲水性,口服吸收好,药代动力学性质得到改善(如氨氟哌酸)。Chu等发现N-1位苯环的引入亦有很好的抗菌活性和优良的药代动力学性质(如双氟哌酸),这可能是由于苯环与喹诺酮母环共轭,产生π-电子效应从而增强了生物活性与组织的分布与吸收。
In recent years, fluoroquinolone antibacterial drugs developed rapidly. Early structure-activity relationship studies have shown that the N-1 substituent is essential for antibacterial activity, such as the introduction of an amino group at the N-1 position which increases hydrophilicity, good oral absorption and improved pharmacokinetic properties such as ammonia Norfloxacin). Chu et al. Found that the introduction of the N-1 benzene ring also has good antibacterial activity and excellent pharmacokinetic properties (such as d x {5e7} o), which may be due to the conjugation of the benzene ring with the quinolone ring to produce π- The electronic effect thus enhances the bioactivity and tissue distribution and absorption.