March L C, Bajwa G S, Lee J, Wasti K, Joullíe M M
J Med Chem. 1976 Jun;19(6):845-8. doi: 10.1021/jm00228a024.
The syntheses of a number of substituted 1,2,4-triazines as potential antimalarials are described. The structural requirements for antimalarial activity are discussed with reference to the substituents of a phenyl group in the 6 position and amino groups at the 3 and 5 positions. Of the compounds tested, 2,5, and 7 produced cures in mice infected with plasmodium berghei. Compounds 2(3,5-diamino-6-(4-trifluoromethylphenyl)-1,2,4-triazine),3,5,8,12,and 37 produced cures in chicks infected with Plasmodium gallinaceum.
本文描述了多种作为潜在抗疟药的取代1,2,4 -三嗪的合成方法。参照6位苯基和3、5位氨基的取代基,讨论了抗疟活性的结构要求。在所测试的化合物中,2、5和7对感染伯氏疟原虫的小鼠产生了治愈效果。化合物2(3,5 -二氨基 - 6 -(4 -三氟甲基苯基)- 1,2,4 -三嗪)、3、5、8、12和37对感染鸡疟原虫的雏鸡产生了治愈效果。