申请人:Yamanouchi Pharmaceutical Co., Ltd.
公开号:US03951954A1
公开(公告)日:1976-04-20
The oxofuryl ester derivatives of 6-(.alpha.-amino-phenylacetamido)penicillanic acid, 7-(.alpha.-aminophenylacetamido)-cephalosporanic acid, or 7-(.alpha. -aminophenylacetamide)desacetoxycephalosporanic acid represented by the general formula ##SPC1## Wherein A represents ##SPC2## Wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a lower alkyl group, said R.sup.1 and R.sup.2 may form together a 1,3-butadienylene group, R.sup.3 represents a hydrogen atom or an acetoxy group, and Means a single bond or a double bond, and acid addition salts of them. When those compounds are orally administered, they are readily absorbed by the intestines and show antibacterial activity by splitting their ester bonds. The rate of absorption of the compounds by the intestines are higher and the toxic property of them is less than those of known compounds similar to the above compounds.
氧喹酯衍生物6-(α-氨基苯乙酰胺基)青霉素酸、7-(α-氨基苯乙酰胺基)头孢菌素酸或7-(α-氨基苯乙酰胺基)脱乙酰氧头孢菌素酸的一般式表示如下:
其中A代表
其中R^1和R^2,可以相同也可以不同,每个代表氢原子或较低的烷基基团,R^1和R^2可以共同形成1,3-丁二烯基团,R^3代表氢原子或乙酰氧基团,并且表示单键或双键,以及它们的酸盐。当这些化合物口服时,它们很容易被肠道吸收,并通过分解其酯键展示抗菌活性。这些化合物通过肠道吸收的速率更高,其毒性较之已知类似化合物的毒性更低。