Pavlov A Y, Olsufyeva E N, Berdnikova T F, Malkova I V, Preobrazhenskaya M N, Risbridger G D
Institute of New Antibiotics, Russian Academy of Medical Sciences, Moscow.
J Antibiot (Tokyo). 1994 Feb;47(2):225-32. doi: 10.7164/antibiotics.47.225.
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.
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。
