Synthesis and analgesic properties of new 4-arylhydrazone 1-H pyrazole [3,4-b] pyridine derivatives
作者:Maria A. Gaston、Luiza Rosaria S. Dias、Antonio Carlos C. Freitas、Ana Luisa P. Miranda、Eliezer J. Barreiro
DOI:10.1016/0031-6865(96)00012-x
日期:1996.8
successful strategy in the planning of new drugs, we describe in this work the synthesis and the analgesic activity of the new functionalized arylcarbaldehyde 4-(1-phenyl-3-methylpyrazolo[3,4-b]pyridine) hydrazone derivatives 5a-m. These derivatives (5a-m) were synthesized in ca. 45% overall yield, using 4-(1-phenyl-3-methylpyrazolo[3,4-b]pyridinyl) hydrazine 6, as key intermediate. by applying classical synthetic
基于生物立体异构原理,这是规划新药的成功策略,我们在这项工作中描述了新型功能化芳基甲醛4-(1-苯基-3-甲基吡唑并[3,4-b]的合成和止痛活性吡啶)衍生物5a-m。这些衍生物(5a-m)约在合成。使用4-(1-苯基-3-甲基吡唑并[3,4-b]吡啶基)肼6作为关键中间体,总产率为45%。通过应用经典的合成方法在杂环系统的C-4处构建芳基hydr单元。由相应的4-氯-(N-苯基-3-甲基吡唑并[3,4-b]吡啶)衍生物7以非常高的产率制备化合物6。这些新化合物5a的抗伤害感受活性通过在白化病小鼠中由0.6%乙酸溶液腹膜内注射诱发的腹部扭曲测试来评估。化合物5f,5g,