首页> 外国专利> L-Isomers of alpha-ureido-acetamido-cephalosporins - more active against beta-lactamase producing bacteria than corresp. D-isomers

L-Isomers of alpha-ureido-acetamido-cephalosporins - more active against beta-lactamase producing bacteria than corresp. D-isomers

机译:α-脲基-乙酰胺基-头孢菌素的L-异构体-与产生对应于β-内酰胺酶的细菌相比,活性更高。 D异构体

摘要

L-isomers of cephalosporins of formula (I) are new: (where R1 = phenyl, thienyl or furyl; R3 = H, alkyl, phenylalkyl, diphenylalkyl, trialkylsilyl, trialkylsannyl, salt-forming cations, substd. phenylalkyl or CH2OCOR. R = alkyl, phenyl or phenylalkyl, the last 2 opt. substd. on the ring by halo, alkyl or alkoxy. R4 is 1-R5-1H-tetrazol-5-yl, 2-R5-1,3,4-thiadiazol-5-yl, 2-R5-1,3,4-oxadiazol-5-yl, 3-R5-1,2,4-thiadiazol-5-yl, 1,2,3,4-thiatriazol-5-yl, R5-substd. isothiazol-5-yl, R5 - substd. isoxazol-5-yl or N-oxypyrid-2-yl. R5 = H or 1-4C alkyl. All 'alkyl' etc. are '-ower'). They are prepd. e.g. by reacting the appropriate alpha-aminoacetamido cpd. with an alkali(ne earth) cyanate. (I) are broad-spectrum antibacterials effective against Gram negative and positive species. They are more effective than the corresp. D-isomers of D,L-racemates against bacteria which produce beta-lactamase e.g. Enterobacter, indole-positive Proteus, resistant E.coli and Serratia. A typical cpd. is 7beta- (aminocarbonyl)amino (L-2-thienyl)acetyl amino -3- (1-m- ethyl-1H-tetrazol-5-yl)thio methyl -8-oxo-5-thia-1-azabicyclo 4,2- ,0 oct-2-ene-2-carboxylic acid.
机译:式(I)的头孢菌素的L-异构体是新的:(其中R 1 =苯基,噻吩基或呋喃基; R 3 = H,烷基,苯基烷基,二苯基烷基,三烷基甲硅烷基,三烷基s基,成盐阳离子,取代苯基烷基或CH 2 OCOR。烷基,苯基或苯基烷基,在环上最后两个最佳被卤素,烷基或烷氧基取代R4为1-R5-1H-四唑-5-基,2-R5-1、3、4-噻二唑-5 -R基,2-R5-1,3,4-恶二唑-5-基,3-R5-1,2,4-噻二唑-5-基,1,2,3,4-噻三唑-5-基,R5 -异噻唑-5-基,R 5-异恶唑-5-基或N-氧吡啶-2-基。R5 = H或1-4C烷基。所有“烷基”等都是“-低级”)。他们准备好了。例如通过使适当的α-氨基乙酰胺基cpd反应与碱金属(氰酸)氰酸盐。 (I)是有效对抗革兰氏阴性和阳性菌种的广谱抗菌剂。它们比正确的方法更有效。 D,L-外消旋物的D-异构体对产生β-内酰胺酶例如细菌的细菌的D。肠杆菌,吲哚阳性变形杆菌,抗性大肠杆菌和沙雷氏菌。典型的cpd。是7β-(氨基羰基)氨基(L-2-噻吩基)乙酰基氨基-3-(1-间乙基-1H-四唑-5-基)硫代甲基-8-氧代-5-硫杂-1-氮杂双环4, 2-,0-辛-2-烯-2-羧酸。

著录项

  • 公开/公告号PT66272A

    专利类型

  • 公开/公告日1977-03-01

    原文格式PDF

  • 申请/专利权人 SQUIBB E R & SONS INC;

    申请/专利号PT19770066272

  • 发明设计人

    申请日1977-03-07

  • 分类号C07D501/36;

  • 国家 PT

  • 入库时间 2022-08-23 00:45:15

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