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新型6β-磺酰胺基青霉烷酸的合成及其β-内酰胺酶抑制活性

Synthesis and beta-lactamase inhibitory activity of new 6 beta-sulfonamidopenicillanic acids.

作者信息

Changov L S, Vassileva-Lukanova B K, Angelova-Galabova A, Pavlova A V, Spassov S L

机构信息

Chemical Pharmaceutical Research Institute, Bulgarian Academy of Sciences, Sofia.

出版信息

Arzneimittelforschung. 1994 Jul;44(7):856-8.

PMID:7945522
Abstract

New 6 beta-aryl(alkyl)sulfonamidopenicillanic acids and their sulfoxides were synthesized by sulfonylation of 6 beta-aminopenicilanic acid or its beta-sulfoxide with an appropriate sulfonyl chloride. The corresponding 6 beta-sulfonamidopenicillanic acids sulfones were prepared by oxidation of the sulfoxides with potassium permanganate in aqueous medium. The obtained compounds reduced the minimum inhibitory concentrations of ampicillin against 8 reference and 7 clinically isolated strains.

摘要

通过用适当的磺酰氯对6β-氨基青霉烷酸或其β-亚砜进行磺酰化反应,合成了新型6β-芳基(烷基)磺酰胺基青霉烷酸及其亚砜。在水介质中用高锰酸钾氧化亚砜制备了相应的6β-磺酰胺基青霉烷酸砜。所得到的化合物降低了氨苄西林对8株参考菌株和7株临床分离菌株的最低抑菌浓度。

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