The novel positively charged pro-drugs of beta-lactam antibiotics in the general 'Structure 4' were designed. The positively charged amino group of the pro-drug not only makes the drugs soluble in water, but also bonds to the negative charge on the phosphate head group of membranes. This bonding will disturb the membrane a little bit and may make some room for the lipophilic portion of the prodrug. The prodrugs can be used medicinally in treating beta-lactam antibiotics-treatable conditions in humans or animals. The prodrugs can be administered transdermally for any kind of medical treatments. Controlled transdermal administration systems of the prodrug enables beta-lactam antibiotics to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of beta-lactam antibiotics.
我们设计出了一般 "结构 4 "中的新型带正电荷的β-内酰胺类抗生素原药。原药带正电荷的
氨基不仅能使药物溶于
水,还能与膜上
磷酸头基的负电荷结合。这种结合会稍微扰乱膜,并为原药的亲脂部分腾出一些空间。原药可用于治疗人类或动物体内可通过β-内酰胺类抗生素治疗的疾病。原药可以透皮给药,用于任何类型的医疗。原药的可控透皮给药系统可使β-内酰胺类抗生素不断达到最佳治疗血药浓度,从而提高疗效并减少β-内酰胺类抗生素的副作用。