Miroshnikova O V, Berdnikova T F, Olsufyeva E N, Pavlov A Y, Reznikova M I, Preobrazhenskaya M N, Ciabatti R, Malabarba A, Colombo L
Institute of New Antibiotics, Russian Academy of Medical Sciences, Moscow, Russia.
J Antibiot (Tokyo). 1996 Nov;49(11):1157-61. doi: 10.7164/antibiotics.49.1157.
An Edman degradation of the antibiotic eremomycin aglycone produced the corresponding hexapeptide, which was aminoacylated with D-lysine, D-histidine or D-tryptophan derivatives to give new heptapeptide analogs of the eremomycin aglycone. The aminoacylation of the eremomycin aglycone produced an octapeptide analog. The substitution of D-lysine for the N-terminal N-methyl-D-leucine does not seriously affect the in vitro antibacterial properties of the eremomycin aglycone whereas the heptapeptides with the N-terminal D-tryptophan or D-histidine moieties and the octapeptide with the N-terminal D-lysine are practically devoid of the antibacterial properties.
对抗生素埃瑞莫霉素苷元进行埃德曼降解反应，得到相应的六肽，该六肽再与D-赖氨酸、D-组氨酸或D-色氨酸衍生物进行氨酰化反应，从而得到埃瑞莫霉素苷元的新型七肽类似物。埃瑞莫霉素苷元的氨酰化反应产生了一种八肽类似物。用D-赖氨酸取代N端的N-甲基-D-亮氨酸对埃瑞莫霉素苷元的体外抗菌性能影响不大，而N端带有D-色氨酸或D-组氨酸部分的七肽以及N端带有D-赖氨酸的八肽实际上没有抗菌性能。
