自研制出头孢呋新甲酯(Cefuroximeaxetil)以来,已报道了许多前药——高效口服的头孢菌素酯类,该类化合物的特点是在头孢核C-7位接有一个氨噻侧链,而主要区别是C-3位取代基不同。我们曾在口服吸收良好的头孢氨节-头孢羟氨苄系列中开发出3-烯头孢菌素,并对3-(2)-丙烯衍生物BMY-28100进行了临床评价。在开发广谱口服头孢菌素的研究过程中,我们在氨噻头孢菌素的C-3位接上烯基侧链,并且确证是一种新的3-(2)-丙烯基头孢菌素BMY-28232(图1)BMY-28232抗菌谱广,对革蓝氏阳性与阴性菌(包括产生β-内酰胺酶的菌株)均有活性, Since cefuroxime axetil has been developed, many prodrugs have been reported as highly effective oral cephalosporins, which are characterized by the attachment of a thiazole side chain at the C-7 position of cephalosporin , While the main difference is that the C-3 substituent is different. We have developed 3-cephalosporin in the well-absorbed Cefaclor cefadroxil series and the clinical evaluation of 3- (2) -propylene derivative BMY-28100. In the development of a broad-spectrum oral cephalosporin study, we linked the alkenyl side chain to the C-3 position of the cephalothin and confirmed to be a novel 3- (2) -propenyl cephalosporin BMY-28232 (Figure 1) BMY-28232 broad antibacterial spectrum of gram-positive and negative bacteria (including β-lactamase-producing strains) are active,