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1-亚甲基-4-萘基偶氮聚合物衍生物的合成与生物学试验

[Synthesis and biological trial of 1-methylene-4-naphthylazo polymer derivates].

作者信息

Korolkovas A, Pellegrino J, Yang G N

出版信息

Rev Farm Bioquim Univ Sao Paulo. 1975 Jul-Dec;13(2):227-36.

PMID:1233592
Abstract

With the purpose of preparing latent forms of six naphthylazoderivatives (five of them are schistosomicidal agents), polymers of these chemotherapeutic agents were synthesized in a two-step reaction. First, polymeric 1-methyleneaminonaphthalene (II) was synthesized by condensing 1-naphthylamine with formaldehyde. Subsequently, coupling of II with five sulfonamides (of which four are moieties of schistosomicidal agents) and 5-aminouracil (which is a part of another schistosomidical agent) yielded polymeric 1-methyleneamino-4-naphthylazoderivaties (IIIa-f). In bioligical tests in mice experimentally infected by Schistosoma mansoni, the six new polymers were found inactive.

摘要

为了制备六种萘基偶氮衍生物(其中五种是杀血吸虫剂)的潜在形式,通过两步反应合成了这些化疗剂的聚合物。首先,通过使1-萘胺与甲醛缩合合成了聚合的1-亚甲基氨基萘(II)。随后,II与五种磺酰胺(其中四种是杀血吸虫剂的部分)和5-氨基尿嘧啶(其是另一种杀血吸虫剂的一部分)偶联,得到聚合的1-亚甲基氨基-4-萘基偶氮衍生物(IIIa-f)。在对实验感染曼氏血吸虫的小鼠进行的生物学试验中,发现这六种新聚合物没有活性。

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