首页> 外国专利> 7-2-2-Amino-4-thiazolyl 2-hydroxy:imino-acetamido 3-cephem derivs. - 3-substd. by alkoxy- or alkyl-thio-methyl are antibiotics active against gram positive and gram negative bacteria

7-2-2-Amino-4-thiazolyl 2-hydroxy:imino-acetamido 3-cephem derivs. - 3-substd. by alkoxy- or alkyl-thio-methyl are antibiotics active against gram positive and gram negative bacteria

机译:7-2-2-氨基-4-噻唑基2-羟基:亚氨基-乙酰氨基3-头孢衍生。 -3减。烷氧基或烷基硫代甲基的抗生素对革兰氏阳性和革兰氏阴性细菌有活性

摘要

(A) 3-R1-X-CH2- 7-( 2-(2-amino-thiazol-4-yl) -2-R-O-N=acetamido 3-cephem-4-COOA derivs. as the syn isomers and their S-oxides of formula (I) and their acid addition salts are new, (where R is H, opt. branched alkyl, alkenyl, alkynyl or cycloalkyl (having at most 6C atoms), acyl (each of the radicals being opt. substd.) or alkoxycarbonyl; A is H, an equivalent of an alkali or alkaline-earth metal, magnesium, ammonium, an aminated organic base or an easily removable ester gp; R1 is alkyl opt. interrupted by a heteroatom, alkenyl or alkynyl (having a maximum of 6C atoms and opt. branched) or opt. substd. aralkyl; X is S, SO, SO2 or O and n is 0, 1 or 2. Antibiotics active against gram-positive bacteria (staphylococci and streptococci, esp. penicillin-resistant staphylococci) and gram negative bacteria (coleform bacteria, klebsiella, salmonella, proteus etc.). They are used to treat infections, such as septic wounds, bronchopneumonia, pulmonary infections, anthrax, septicaemia etc. by oral, rectal, parenterol or topical application. MIC tests and in vivo tests in mice are described.
机译:(A)3-R1-X-CH2-7-(2-(2-氨基-噻唑-4-基)-2-RON =乙酰氨基3-cephem-4-COOA衍生为顺式异构体及其S-式(I)的氧化物及其酸加成盐是新的(其中R为H,优选为支链烷基,烯基,炔基或环烷基(具有至多6个碳原子),酰基(每个基团均被优选取代)。 A为氢,相当于碱金属或碱土金属,镁,铵,胺化有机碱或易除去的酯gp; R1为被杂原子,烯基或炔基间断的烷基(最大碳原子数为6C的原子且选择为支链)或选择取代为芳烷基; X为S,SO,SO2或O,n为0、1或2。抗生素对革兰氏阳性细菌(葡萄球菌和链球菌,尤其是耐青霉素的细菌)有效葡萄球菌)和革兰氏阴性细菌(大肠菌,克雷伯菌,沙门氏菌,变形杆菌等),用于口服治疗感染,如化脓性伤口,支气管肺炎,肺部感染,炭疽,败血病等。 ,直肠,肠胃外或局部应用。描述了小鼠的MIC测试和体内测试。

著录项

  • 公开/公告号FR2499995B1

    专利类型

  • 公开/公告日1985-01-18

    原文格式PDF

  • 申请/专利权人 ROUSSEL UCLAF;

    申请/专利号FR19810006736

  • 发明设计人

    申请日1981-04-03

  • 分类号C07D501/24;A61K31/545;

  • 国家 FR

  • 入库时间 2022-08-22 07:56:10

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