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[带有乙醛酰苯腙侧链的新型氨苄青霉素衍生物]

[New ampicillin derivatives with glyoxyloylbenzhydrazone side chains].

作者信息

Heinisch L, Hanschke K G, Willitzer H, Möllmann U, Tresselt D, Stengel K, Eckardt K, Kleinwächter W

机构信息

Institut für Mikrobiologie und experimentelle Therapie (ZIMET), Jena.

出版信息

Pharmazie. 1992 Jun;47(6):412-5.

PMID:1409839
Abstract

New ampicillin derivatives were synthesized from glyoxylic acid benzhydrazones by reaction with chloroformates via mixed anhydrides and ampicillin. These compounds were tested in an agar diffusion test against six different bacterial strains and also for their stability against beta-lactamases. Studies about structure-activity relationships have shown, that the activity against different bacterial strains is influenced in different manner by hydrophilic or hydrophobic and electronic properties of substituents.

摘要

通过乙二醛苯腙与氯甲酸酯经混合酸酐反应以及与氨苄西林反应合成了新的氨苄西林衍生物。这些化合物在琼脂扩散试验中针对六种不同的细菌菌株进行了测试,并且还测试了它们对β-内酰胺酶的稳定性。关于构效关系的研究表明,取代基的亲水或疏水以及电子性质以不同方式影响对不同细菌菌株的活性。

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