申请人:Bayer Aktiengesellschaft
公开号:US03931153A1
公开(公告)日:1976-01-06
Penicillins of the formula: ##SPC1## And their pharmaceutically acceptable nontoxic salts wherein R.sub.1 is hydrogen, halogen, lower alkyl, hydroxy, nitro or A--NH; A is ##EQU1## wherein R.sub.3 is hydrogen; lower alkyl; halo-(lower alkyl); cycloalkyl of 3 to 11 carbon atoms, unsubstituted or substituted by hydroxy or alkyl of 1 or 2 carbon atoms; cycloalkenyl of 3 to 11 carbon atoms; bicycloalkyl of up to 8 carbon atoms; bicycloalkenyl of up to 8 carbon atoms; aryl of 6 to 10 carbon atoms, unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, trifluoromethyl, nitro, amino, alkylsulphonyl of 1 to 4 carbon atoms, and methylenedioxy; azidoaryl of 6 to 10 carbon atoms, azido-(lower alkyl); amino; or thienyl; R.sub.4 is lower alkylamino or arylamino of 6 to 10 carbon atoms; B is a direct bond; CH.sub.2 ; S--CH.sub.2 ; CH=CH; or CO--NH--CH.sub.2 ; E is phenyl or phenyl or thenyl, substituted by hydroxy, azido, lower alkyl, lower alkoxy, lower alkylthio or chlorine; and C* is an asymmetric carbon atom, Are useful for their antibacterial activity against both Gram-positive and Gram-negative bacteria.
公式为:##SPC1## 的青霉素及其药学上可接受的无毒盐,其中 R.sub.1 是氢、卤素、较低的烷基、羟基、硝基或 A--NH;A 是 ##EQU1## 其中 R.sub.3 是氢;较低的烷基;卤代-(较低的烷基);3到11个碳原子的环烷基,未取代或取代为羟基或1或2个碳原子的烷基;3到11个碳原子的环烯基;多环烷基,最多含8个碳原子;多环烯基,最多含8个碳原子;6到10个碳原子的芳基,未取代或取代为1到3个取代基,所述取代基选自1到4个碳原子的烷基、1到4个碳原子的烷氧基、卤素、三氟甲基、硝基、氨基、1到4个碳原子的烷基磺酰基和亚甲二氧基;6到10个碳原子的偶氮芳基,偶氮-(较低的烷基);氨基;或噻吩基;R.sub.4 是6到10个碳原子的较低的烷基氨基或芳基氨基;B 是直接键;CH.sub.2;S--CH.sub.2;CH=CH;或 CO--NH--CH.sub.2;E 是苯基或苯基或噻吩基,取代为羟基、偶氮基、较低的烷基、较低的烷氧基、较低的烷基硫基或氯;C* 是一个不对称碳原子,对其抗菌活性对抗革兰氏阳性和阴性细菌均有用。