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

A Korolkovas, J Pellegrino, G N Yang
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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.

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[1-亚甲基-4-萘偶氮聚合物衍生物的合成及生物学试验]。
为了制备六种萘酰唑衍生物(其中五种是杀血吸虫剂)的潜伏形式,用两步法合成了这些化疗药物的聚合物。首先,将1-萘胺与甲醛缩合,合成了聚合物1-亚甲基氨基萘(II)。随后,II与五种磺胺(其中四种是杀血吸虫剂的部分)和5-氨基尿嘧啶(另一种血吸虫剂的一部分)偶联,产生聚合物1-亚甲基氨基-4-萘酰衍生物(IIIa-f)。在曼氏血吸虫实验感染小鼠的生物学试验中,发现六种新聚合物无活性。
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