Korolkovas A, Pellegrino J, Romero J R, Goncalez E J
Rev Farm Bioquim Univ Sao Paulo. 1975 Jul-Dec;13(2):217-25.
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.
五种萘基偶氮衍生物(磺胺嘧啶、磺胺二甲嘧啶、磺胺噻唑、磺胺甲恶唑和磺胺间甲氧嘧啶)——前四种具有杀血吸虫活性——通过使这些化合物与丙烯酸和甲基丙烯酸的聚合物反应,以聚酰胺的形式被潜伏化。在对实验感染曼氏血吸虫的小鼠进行的生物学测试中,发现这九种新化合物没有活性。然而,本文所述的原始潜伏化方法具有广泛应用的可能性,这归因于其有利特性:聚合物反应基团的多功能性、药物与聚合物之间形成的键的不稳定性(易于水解)、聚酐与药物之间反应的更高活性以及由此形成的聚合物在水中的溶解性。