氨基嘧啶烷磺酸衍生物的合成及其抗病毒活性的研究

Studies on the Synthesis and Antiviral Activity of Aminopyrimidine Alkylsulphonic Acid Derivatives

本文提供合成3-(2.6—二氯—4一氨基嘧啶基)一丙烷-1-磺酸的方法,以氰基乙酸乙酯与尿素为原料进行缩合,再经氯化与烷磺酸化而得。所得化合物具性质稳定、水溶性好的优点。经细胞试验与动物试验证明了它具抗单纯疱疹病毒、牛痘苗病毒、腺病毒8型等的活性。其抑毒活性与三氮唑核苷及无环乌苷相近。

The 3-(2, 6-dichloro-4-pyrimidylamino)-propan-l-sulphonic acid is pre- pared by the condensation of ethyl cyanoacetate and urea, and then by chlorination and alkylsulphonation. It is stability in use and solubility in water. The experiment in cell cultures and in animals has proved that it is active as antiviral agent against the Herpes Simplex, Vanccinia virus and Adeno virus-8. The antiviral effect is simi- lar to Virazole and Acyclovir.