李志裕 陆平波 季 晖 邵 卿 尤启冬 刘 潇. 苯基四氮唑类化合物的合成与抗组胺释放活性研究J. 药学学报, 2009,44(10): 1112-1117.
引用本文: 李志裕 陆平波 季 晖 邵 卿 尤启冬 刘 潇. 苯基四氮唑类化合物的合成与抗组胺释放活性研究J. 药学学报, 2009,44(10): 1112-1117.
LI Zhi-Yu, Liu-Beng-Bei, Ji- Hui, Shao- Qing, You-Qi-Dong, Liu- Xiao. Synthesis and anti-histamine release activity of phenyl tetrazole compoundsJ. 药学学报, 2009,44(10): 1112-1117.
Citation: LI Zhi-Yu, Liu-Beng-Bei, Ji- Hui, Shao- Qing, You-Qi-Dong, Liu- Xiao. Synthesis and anti-histamine release activity of phenyl tetrazole compoundsJ. 药学学报, 2009,44(10): 1112-1117.

苯基四氮唑类化合物的合成与抗组胺释放活性研究

Synthesis and anti-histamine release activity of phenyl tetrazole compounds

  • 摘要:

    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))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NP03compound 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。

     

    Abstract:

    Ongoing effort to find novel antiasthmatic drugs led to the design and synthesis of a series of compounds bearing phenyl tetrazole group based on the SAR study.  The important intermediate 3-(1H-tetrazol-5- yl) benzenamine was synthesized from m-nitroaniline via cyclization and hydrogenation. Followed by amidation, eight new target compounds were obtained.  The structures of these compounds were confirmed with 1H NMR, ESI-MS and elemental analysis.  Their non-specific and specific anti-histamine effects in the mast cell were  determined.  Compound NP03 could inhibit non-specific histamine release induced by compound 48/80 in mast cell of SD rats.

     

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