为寻找疗效更好的抗过敏哮喘药物,本文在对该类药物构效关系研究的基础上,以塔赞司特为先导化合物,设计并合成了酰胺基苯基四氮唑类化合物。以间硝基苯腈为原料,经环合、氢化还原得重要中间体3-(5-(1H-四氮唑)基)苯胺,最后经酰胺化反应共合成了8个目标化合物,化合物结构经核磁、质谱、元素分析确证,并对其进行了非特异及特异性抗组胺活性研究。其中化合物NP03对compound 48/80诱导的SD大鼠肥大细胞非特异性组胺释放的抑制作用与阳性对照药相当。 In order to find out more effective antiallergic asthma drugs, based on the structure-activity relationship of these drugs, we designed and synthesized amidophenyltetrazole compounds using tazostat as the lead compound. Nitrobenzonitrile was used as the starting material to cyclize and hydrogenate to obtain 3- (5- (1H-tetrazolium)) aniline which is an important intermediate. Finally, 8 target compounds were synthesized by amidation reaction. The structures of the compounds The results of nuclear magnetic resonance, mass spectrometry and elemental analysis confirmed the non-specific and specific anti-histamine activity. The compound NP03 inhibited the compound 48/80-induced non-specific histamine release from mast cells in SD rats in a similar manner as the positive control.