Zhou W C, Xin Z M, Zhang X P, Shen J, Qiu Q P
Shanghai Institute of Pharmaceutical Industry.
Yao Xue Xue Bao. 1996;31(11):823-30.
Two series of compounds, 1,2-dihydro-2,2-dimethyl-4, 6-diamino-1-(omega-haloalkyloxy)-s-triazines and O, O'-bis (4, 6-diamino-1, 2-dihydro-2, 2-disubstituted-s-triazin-l-yl) alkanediols were synthesized and tested against Plasmodium berghei and Trypanosoma evansi in mice. Most title compounds showed good antimalarial activity and compounds IIc-e showed good antitrypanosomal effect. After further studies on pharmacology, toxicology, pharmacokinetics and efficacy on infected cattles compound IIe (SIPI-1029, T-46) was shown to be a new highly active antitrypanosomal agent with low toxicity and long half life in plasma.
合成了两类化合物，即1,2 - 二氢 - 2,2 - 二甲基 - 4,6 - 二氨基 - 1 -（ω - 卤代烷氧基）- s - 三嗪和O，O'-双（4,6 - 二氨基 - 1,2 - 二氢 - 2,2 - 二取代 - s - 三嗪 - 1 - 基）链烷二醇，并在小鼠体内针对伯氏疟原虫和伊氏锥虫进行了测试。大多数目标化合物显示出良好的抗疟活性，化合物IIc - e显示出良好的抗锥虫效果。在对药理学、毒理学、药代动力学以及对感染牛的疗效进行进一步研究后，化合物IIe（SIPI - 1029，T - 46）被证明是一种新型的高效抗锥虫剂，具有低毒性和在血浆中较长的半衰期。
