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通过卤代烷作用对糖肽类抗生素埃瑞霉素进行修饰及对所得化合物抗菌活性的研究。

Modification of glycopeptide antibiotic eremomycin by the action of alkyl halides and study on antibacterial activity of the compounds obtained.

作者信息

Pavlov A Y, Olsufyeva E N, Berdnikova T F, Malkova I V, Preobrazhenskaya M N, Risbridger G D

机构信息

Institute of New Antibiotics, Russian Academy of Medical Sciences, Moscow.

出版信息

J Antibiot (Tokyo). 1994 Feb;47(2):225-32. doi: 10.7164/antibiotics.47.225.

Abstract

Alkylation of glycopeptide antibiotic eremomycin by the action of different alkyl halides leads, depending on the structure of alkyl halides used, to eremomycin derivatives of six types; alkylated at the N-terminus, quaternary compounds at the N-terminus, eremomycin esters, esters of eremocycin alkylated at the N-terminus, esters of eremomycin quaternised at the N-terminus, esters of eremomycin alkylated both at the N-terminus and at the aminogroup of disaccharide branch. Five compounds demonstrated high antibacterial activity in vitro, N-allyleremomycin and methyl ester of N,N-dimethyleremomycin being at least as good as the parent eremomycin.

摘要

在不同卤代烷的作用下,糖肽抗生素埃瑞霉素发生烷基化反应,根据所用卤代烷的结构,会生成六种类型的埃瑞霉素衍生物:N-端烷基化产物、N-端季铵化合物、埃瑞霉素酯、N-端烷基化的埃瑞霉素酯、N-端季铵化的埃瑞霉素酯、N-端和二糖支链氨基均烷基化的埃瑞霉素酯。五种化合物在体外表现出高抗菌活性,N-烯丙基埃瑞霉素和N,N-二甲基埃瑞霉素甲酯的抗菌活性至少与母体埃瑞霉素相当。

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