A method for improving the intestinal absorption of a cephalosporin derivative by bonding an oligopeptide having the general formula (I):
wherein
X is a hydrogen atom, C1-15 alkyl group, R3CO- group wherein R3 is a hydrogen atom or straight or branched chain C1-15 alkyl group or a protective group easily removable by acid hydrolysis, hydrogenolysis or enzyme existing in a living body;
R, and R2 each independently is a side chain of an amino acid constituting the oligopeptide; and
n is integer of 1 to 3, to any side chain at the 3-, 4- or 7-position of a 7-aminocephalosporanic acid derivative having antibacterial activity.
一种通过结合具有通式(I)的寡肽来改善
头孢菌素衍
生物肠道吸收的方法:
其中
X是氢原子、C1-15烷基、R3CO-基团,其中R3是氢原子或直链或支链C1-15烷基或易被活体内存在的酸
水解、氢解或酶去除的保护基团;
R 和 R2 各自独立地是构成寡肽的
氨基酸的侧链;以及
n 为 1 至 3 的整数,为具有抗菌活性的
7-氨基头孢烷酸衍
生物的 3-、4-或 7-位上的任意侧链。