[Latentiation of naphthylazoderivatives by polymerarization].

A Korolkovas, J Pellegrino, J R Romero, E J Goncalez
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引用次数: 0

Abstract

Five naphthylazoderivatives (of sulfadiazine, sulfamethazine, sulfathiazole, sulfamethoxazole, and sulfamonomethoxine) -- the first four displaying schistosomicidal activity -- were latentiated, in the form of polyamides of acrylic and methacrylic acids, by reacting those compounds with these polymers. In biological tests in mice experimentally infected by Schistosoma mansoni, the new nine compounds were found to be inactive. However, the original method of latentiation described in this paper has possibilities of wide application, owing to its favourable features: versatility of the reactive group of the polymer, lability of the bond (easily hydrolyzable) formed between drug and polymer, greater viability of reaction between the polyanhydride and the drug, and solubility in water of the polymers thus formed.

[通过聚合的方法对萘杂化衍生物的影响]。
五种萘酰肼衍生物(磺胺嘧啶、磺胺乙嘧啶、磺胺噻唑、磺胺甲恶唑和磺胺甲氧嘧啶)——前四种显示出杀血吸虫活性——通过与这些聚合物反应,以丙烯酸和甲基丙烯酸聚酰胺的形式被潜伏。在曼氏血吸虫实验感染小鼠的生物学试验中,发现这9种化合物无活性。然而,本文所描述的原始潜伏方法具有以下优点,具有广泛应用的可能性:聚合物的反应基团的通用性,药物与聚合物之间形成的键的不稳定性(易于水解),聚酸酐与药物之间的反应活力更大,以及由此形成的聚合物在水中的溶解度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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