7-芳胺基-3-氰基-5-烷基吡唑并[1,5-a]嘧啶类化合物的合成及药理活性

Synthesis and pharmacological activities of 7-anilino-3-cyano-5-alkyl pyrazolo[1,5-a] pyrimidine derivatives

目的设计并合成7-芳胺基-3-氰基-5-烷基吡唑并[1,5-a]嘧啶类化合物,初步评价其药理活性。方法以丙二腈和原甲酸三乙酯为起始原料,通过新的合成路线制备了目标化合物;采用MTT法测定目标化合物的细胞毒性。结果与结论合成了13个新化合物,其结构经1H-NMR、MS确证,7个化合物显示出不同程度的细胞毒性,化合物8a、8f、8g的活性较好,有进一步研究的价值。

Objective To design and synthesize 7-anilino-3-cyano-5-alkylpyrazolo[ 1, 5-a] pyrimidine deriva- tives and primarily evaluate their pharmacological activity. Methods A new synthetic route was used to synthesize the title compounds starting from malononitrile and triethoxymethane, and their cytotoxicity were examined using MTT method. Results and Conclusion Thirteen new compounds were synthesized and their structures were confirmed by ^1H-NMR and MS. Seven of them showed cytotoxicity, while compounds 8a, 8f and 8g displayed promising activity and were worth further studying.