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氟哌酸(norfloxacin)是吡酮酸类药物的优秀代表之一,其特点是抗菌谱广,抗菌作用强,该药对绿脓杆菌的作用较庆大霉素强,并远优于萘啶酸和吡哌酸,但美中不足的是易于代谢和体内生物利用度及血浓度较低,从而影响了实际效果。为了改善疗效,根据药物在体内作用和代谢以及口服给药的特点,设计合成了系列氟哌酸的新类似物,以期通过改造化合物结构来改变化合物的理化性质,体内代谢途径,获得血浓度和活性高、毒副作用小,疗效更好的抗菌药物。合成路线如下:
Norfloxacin is one of the best representatives of p-keto acids and is characterized by its broad antibacterial spectrum and strong antibacterial activity. The drug has a stronger effect on Pseudomonas aeruginosa than gentamicin and far superior to naphthyridine Acid and pipemidic acid, but the fly in the ointment is the ease of metabolism and in vivo bioavailability and lower blood concentration, thus affecting the actual results. In order to improve the curative effect, a series of new analogs of norfloxacin were designed and synthesized according to the function and metabolism of the drug in the body and the oral administration, in order to change the physicochemical properties of the compound and the metabolic pathways in vivo so as to obtain the blood concentration and High activity, small side effects, better efficacy of antibacterial drugs. The synthetic route is as follows: