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某些脲基头孢氨苄和头孢羟氨苄衍生物的合成及其抗菌活性

Synthesis and antibacterial activity of some ureido cephalexin and cefadroxil derivatives.

作者信息

Valcavi U, Brandt A, Corsi G B, Innocenti S, Minoja F, Pascucci G

出版信息

Farmaco Sci. 1980 Jul;35(7):563-72.

PMID:7450045
Abstract

The antibacterial activity of some ureido, acylureido and carbamoylureido derivatives of cephalexin and cefadroxil, prepared in our laboratories, as compared to parent compounds is reported. Only the 7-[D-alpha-(imidazolidin-2-one-1-ylcarbonylamino)-alpha-phenylacetamido]-3-methyl-3-cephem-4-carboxylic acid (IV d) and the 7-[D-alpha-(imidazolidin-2-one-1-ylcarbonylamino)-alpha-p-hydroxyphenylacetamido]-3-methyl-3-cephem-4-carboxylic acid (V c) showed some antibiotic activity. However we found no activity improvement against Pseudomonas strains (contrary to the results obtained in similar penicillin derivatives) and a lower beta-lactamase resistance.

摘要

据报道,我们实验室制备的头孢氨苄和头孢羟氨苄的一些脲基、酰脲基和氨基甲酰脲基衍生物与母体化合物相比的抗菌活性。只有7-[D-α-(咪唑烷-2-酮-1-基羰基氨基)-α-苯乙酰胺基]-3-甲基-3-头孢烯-4-羧酸(IV d)和7-[D-α-(咪唑烷-2-酮-1-基羰基氨基)-α-对羟基苯乙酰胺基]-3-甲基-3-头孢烯-4-羧酸(V c)表现出一些抗生素活性。然而,我们发现对假单胞菌菌株没有活性提高(与在类似青霉素衍生物中获得的结果相反),并且β-内酰胺酶抗性较低。

相似文献

1
Synthesis and antibacterial activity of some ureido cephalexin and cefadroxil derivatives.某些脲基头孢氨苄和头孢羟氨苄衍生物的合成及其抗菌活性
Farmaco Sci. 1980 Jul;35(7):563-72.
2
Bactericidal activity of cefadroxil, cephalexin, and cephradine in an in vitro pharmacokinetic model.头孢羟氨苄、头孢氨苄和头孢拉定在体外药代动力学模型中的杀菌活性。
J Antibiot (Tokyo). 1979 Jul;32(7):718-26. doi: 10.7164/antibiotics.32.718.
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Evaluation in an animal model and in vitro of the combination clavulanic acid and cephalosporins against beta-lactamase producing and nonproducing Staphylococcus aureus strains.在动物模型和体外对克拉维酸与头孢菌素联合用药针对产β-内酰胺酶和不产β-内酰胺酶的金黄色葡萄球菌菌株进行评估。
Braz J Infect Dis. 2000 Feb;4(1):36-42.
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[Microbiological tests of 2 recent cephalosporins: cefadroxil and cefuroxime].[两种近期头孢菌素的微生物学检测:头孢羟氨苄和头孢呋辛]
Ann Sclavo. 1980 Nov-Dec;22(6):957-63.
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[Bacteriological study on cefadroxil in vitro. Correlation between diameter of inhibition zone and inhibitory concentration (author's transl)].头孢羟氨苄的体外细菌学研究。抑菌圈直径与抑菌浓度之间的相关性(作者译)
Arzneimittelforschung. 1980;30(2):301-3.
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Comparative antibacterial spectrum of cefadroxil.头孢羟氨苄的比较抗菌谱。
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Synthesis and biological activity of novel 3-(2-propenyl)-cephalosporins. I.
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[In vitro and in vivo antimicrobial activity of cefuroxime cefamandole and cephalexin on freshly isolated strains of Gram-positive and Gram-negative bacteria].
Boll Soc Ital Biol Sper. 1981 Jul 15;57(13):1450-6.
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Comparison of pharmacological and antimicrobial properties of cefadroxil and cephalexin.头孢羟氨苄与头孢氨苄的药理及抗菌特性比较。
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