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7-Thiazolidine-carboxamido-cephalosporin cpds. - useful as antibacterial agents, have good penicillinase resistance

机译:7-噻唑烷-羧酰胺基-头孢菌素cpds。 -用作抗菌剂,对青霉素酶具有良好的抵抗力

摘要

Cephalosporins of formula (I) and their optical isomers and accid-addn. salts are new. (where R is H, 1-4C alkyl, aralkyl, phenyl, halo- or methoxyphenyl, CHO, acyl or trimethylsilyl; R' is H, a cation, 1-4C alkyl, CH2CCl3, acetonyl, benzyl, nitro or methoxymethyl, pivaloyloxymethyl, phthalidyl, benzoyloxymethyl, 5-indanyl, CH(Me)OCOOEt or CH2NHCOR", where R" is 1-4C alkyl, 5-6C cycloalkyl or aryl, or R' is a negative charge when A is pyridinio; A is H, halogen, N3, OH, NH2, pyridinio, OCONH2, OR1, OCOR1, NHCOR1 or SR1, where R1 is 1-5C alkyl, opt. substd. aryl or opt. substd. heterocyclyl; n=0 or 1). (I) have antibacterial activity against Gram-positive and -negative bacteria (including beta- lactamase-producing strains) and good penicillinase resistance. They can be used in human and veterinary medicine, as antiseptics and disinfectants, and for controlling bacterial diseases of plants.
机译:式(I)的头孢菌素及其旋光异构体和accid-addn。盐是新的。 (其中R是H,1-4C烷基,芳烷基,苯基,卤代或甲氧基苯基,CHO,酰基或三甲基甲硅烷基; R'是H,阳离子,1-4C烷基,CH2CCl3,丙酮基,苄基,硝基或甲氧基甲基,新戊酰氧基甲基,苯二甲酰基,苯甲酰氧基甲基,5-茚满基,CH(Me)OCOOEt或CH2NHCOR“,其中R”是1-4C烷基,5-6C环烷基或芳基,或当A是吡啶基时,R'是负电荷; A是H,卤素,N 3,OH,NH 2,吡啶基,OCONH 2,OR 1,OCOR 1,NHCOR 1或SR 1,其中R 1为1-5 C烷基,优选为芳基或优选为杂环基; n = 0或1)。 (I)对革兰氏阳性和阴性细菌(包括产生β-内酰胺酶的菌株)具有抗菌活性,并对青霉素酶具有良好的抗性。它们可以在人类和兽医学中用作防腐剂和消毒剂,并用于控制植物的细菌病。

著录项

  • 公开/公告号PT74230A

    专利类型

  • 公开/公告日1982-01-02

    原文格式PDF

  • 申请/专利权人 AUSONIA FARMACEUTICI SRL;

    申请/专利号PT19810074230

  • 发明设计人 VITTORIA ORRU;MICHEL DI SCHIENA;

    申请日1981-12-30

  • 分类号C07D;A61K;

  • 国家 PT

  • 入库时间 2022-08-22 13:37:32

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