申请人:Bayer Aktiengesellschaft
公开号:US04107304A1
公开(公告)日:1978-08-15
Cephalosporins of the formula ##STR1## their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, wherein A is hydrogen; unsubstituted or substituted alkyl; aryl; or R.sub.1 --X--, wherein X is --CO-- or --SO.sub.2 --, and R.sub.1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl; Or when X is --CO--, R.sub.1 can also be alkoxy; B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety ##STR2## E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality. These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.
根据上述公式制备头孢菌素及其药学上可接受的、无毒的盐和水合物,其中A是氢;未取代或取代的烷基;芳基;或R.sub.1--X--,其中X是--CO--或--SO.sub.2--,而R.sub.1是氢,未取代或取代的烷基;芳基;噻吩基;呋喃基;氨基;烷基氨基;二烷基氨基;吡咯烷基;或哌啶基;或当X是--CO--时,R.sub.1还可以是烷氧基;B是苯基,甲基苯基,氯苯基,羟基苯基或上述的结构;E是氢,羟基或乙酰氧基;C是一个手性中心。这些化合物特别适用于其抗微生物和特别是抗菌作用。