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    • 6. 发明授权
    • Penicillins
    • 青霉素
    • US4008220A
    • 1977-02-15
    • US495914
    • 1974-08-08
    • Hisao TobikiHirotada YamadaIwao NakatsukaKozo ShimagoShigeru OkanoTakenari NakagomeToshiaki KomatsuAkio IzawaHiroshi NoguchiYasuko Eda
    • Hisao TobikiHirotada YamadaIwao NakatsukaKozo ShimagoShigeru OkanoTakenari NakagomeToshiaki KomatsuAkio IzawaHiroshi NoguchiYasuko Eda
    • C07D499/00C07D499/68C07D499/48
    • C07D499/00Y02P20/55
    • A penicillin of the formula: ##STR1## wherein ##STR2## is a six-membered heteroaromatic ring containing 1 or 2 nitrogen atoms as the hetero atom, Y is hydrogen, lower alkanoyl or lower alkoxycarbonyl, R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkanoyl, benzoyl, lower alkylmercapto, hydroxyl, mercapto, hydroxy(lower)alkyl, halogen or cyano or R.sub.1 and R.sub.2 may link together to form a lower alkylene chain which may be substituted with an oxo group, and Z is phenyl, hydroxyphenyl, lower alkyl, cyclohexadienyl, thienyl or isothiazolyl, which is prepared by reacting a compound of the formula: ##STR3## wherein Z is as defined above or its derivative with a carboxylic acid of the formula: ##STR4## wherein ##STR5## and R.sub.2 are each as defined above or its reactive derivative, if necessary, followed by hydrolysis or acylation of the resulting product and/or elimination of any protective group and which is useful as an antimicrobial agent against various gram-positive and gram-negative bacteria including Pseudomonas.
    • 一种下式的青霉素:其中是含有1或2个氮原子作为杂原子的六元杂芳环,Y是氢,低级烷酰基或低级烷氧基羰基,R 1和R 2各自是氢,低级烷基 ,低级烷酰基,苯甲酰基,低级烷基巯基,羟基,巯基,羟基(低级)烷基,卤素或氰基,或者R 1和R 2可以连接在一起形成可被氧代基取代的低级亚烷基链,Z是苯基, 低级烷基,环己二烯基,噻吩基或异噻唑基,其通过使下式化合物:其中Z如上所定义或其衍生物与下式的羧酸反应制备:其中和R2 各自如上所定义,或其反应性衍生物,如果需要,随后水解或酰化所得产物和/或消除任何保护基团,并且其可用作针对各种革兰氏阳性和革兰氏阴性菌的抗微生物剂,包括 uding假单胞菌
    • 7. 发明授权
    • Penicillins substituted with heterocyclic and substituted phenyl groups
    • 用杂环和取代的苯基取代的青霉素
    • US3992371A
    • 1976-11-16
    • US536181
    • 1974-12-24
    • Hisao TobikiHirotada YamadaIwao NakatsukaKozo ShimagoShigeru OkanoTakenari NakagomeToshiaki KomatsuAkio IzawaHiroshi NoguchiYasuko Eda
    • Hisao TobikiHirotada YamadaIwao NakatsukaKozo ShimagoShigeru OkanoTakenari NakagomeToshiaki KomatsuAkio IzawaHiroshi NoguchiYasuko Eda
    • C07D499/10C07D471/04C07D499/00C07D499/04C07D499/64C07D499/68C07D519/06C07D499/70
    • C07D471/04C07D499/00
    • Novel penicillins of the formula ##SPC1##Wherein ##EQU1## represents a substituted or unsubstituted benzene or nitrogen atom-containing heteroaromatic ring which may be substituted, ##EQU2## represents a pyridine, pyrazine or pyridazine ring, X represents an oxygen or sulfur atom, Y represents a hydrogen atom or a loer alkoxycarbonyl or lower alkanoyl group, and R.sub.1, R.sub.2 and R.sub.3 are each a hydrogen or halogen atom or a nitro, lower alkylamino, di(lower)alkylamino, aine, lower alkoxycarbonylamino, lower alkanoylamino, amino(lower)alkyl, lower alkyl, lower alkoxy, hydroxyl, sulfamoyl, trifluoromethyl, lower alkylthio or lower alkylsulfonyl group, excluding the cases where all of R.sub.1, R.sub.2 and R.sub.3 are hydrogen atoms and where R.sub.1 is a hydroxyl group and R.sub.2 and R.sub.3 are each a hydrogen or halogen atom, and their nontoxic, pharmaceutically acceptable salts, which can be prepared by reacting a carboxylic acid of the formula: ##EQU3## wherein ##EQU4## X and Y are each as defined above or its reactive derivative with a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2 and R.sub.3 are each as defined above or its reactive derivative, and are ueful as antimicrobial agents against gram-positive and gram-negative bacteria including Pseudomonas.
    • 式+ q,10的新型青霉素其中C | A C表示可被取代的取代或未取代的含有苯或含氮原子的杂芳环,C | C | CB表示吡啶,吡嗪或哒嗪环,X表示 氧或硫原子,Y表示氢原子或低级烷氧基羰基或低级烷酰基,R 1,R 2和R 3各自为氢或卤素原子或硝基,低级烷基氨基,二(低级)烷基氨基,亚氨基,低级烷氧基羰基氨基, 低级烷酰基氨基,氨基(低级)烷基,低级烷基,低级烷氧基,羟基,氨磺酰基,三氟甲基,低级烷硫基或低级烷基磺酰基,不包括R1,R2和R3全部为氢原子,其中R1为羟基, R2和R3各自为氢或卤素原子,以及它们的无毒的药学上可接受的盐,其可以通过使下式的羧酸:XY | C | C-COOH A | CB反应而制备,其中CC | | CA | | C,CB,X和Y为ea ch或其反应性衍生物与下式的化合物:+ q,21,其中R1,R2和R3各自如上所定义,或其反应性衍生物,并且作为抗革兰氏阳性和革兰氏阴性细菌的抗微生物剂 包括假单胞菌。