Shepelevtsev N G, Gol'dberg L E, Olsuf'eva E N, Povarov L S
Antibiotiki. 1982 Jan;27(1):57-61.
Synthesis of 2 new N-acyl derivatives of carminomycin and rubomycin (N-L-leucylcarminomycin and N-sarcolysylrubomycin) is described. Acute toxicity of the new and 4 known N-acyl derivatives: N-acetylcarminomycin, N,L-alanylcarminomycin, N-D-phenylalanylcarminomycin and N-D-phenylalanylrubomycin was studied on albino mice. It was shown that the N-acyl derivatives of carminomycin and rubomycin had lower acute toxicity than the initial drugs. When added to blood serum in vitro N-D-phenylalanylcarminomycin and N-D-phenylalanylrubomycin induced precipitation. The carminomycin derivatives containing the residues of L-leucine and L-alanine were less toxic than the initial antibiotic, still they had a markedly pronounced retarded toxicity.
本文描述了两种新的洋红霉素和柔红霉素的N-酰基衍生物(N-L-亮氨酰洋红霉素和N-肌氨酸酰柔红霉素)的合成。研究了这两种新的以及4种已知的N-酰基衍生物:N-乙酰洋红霉素、N,L-丙氨酰洋红霉素、N-D-苯丙氨酰洋红霉素和N-D-苯丙氨酰柔红霉素对白化小鼠的急性毒性。结果表明,洋红霉素和柔红霉素的N-酰基衍生物的急性毒性低于初始药物。体外加入血清时,N-D-苯丙氨酰洋红霉素和N-D-苯丙氨酰柔红霉素会引起沉淀。含有L-亮氨酸和L-丙氨酸残基的洋红霉素衍生物毒性低于初始抗生素,但其仍具有明显的延迟毒性。