二芳甲基哌嗪衍生物合成及其抗组胺活性的研究

Synthesis and Antihistaminic Activity of Diarylmethylpiperazine Derivatives

目的利用电子等排和拼合原理,选择H_1受体拮抗剂的活性部分二芳甲基哌嗪与白三烯受体拮抗剂的活性结构色酮-2-羧酸拼接,设计合成二芳甲基哌嗪衍生物,并且考察其抗组胺活性。方法以羟基取代的色酮-2-羧酸酯为母体,将羟基与二芳甲基哌嗪通过脂肪链相连,得二芳甲基哌嗪衍生物,并测定化合物的抗组胺活性。结果目标化合物的组成和结构经质谱和核磁共振氢谱确认。

Objective The diarylmethylpiperazine moiety as active group frequently existing in the structures of H1 receptor antagonists and chromone-2-carboxylic acid moiety as active structure existing in leukotriene receptor antagonists were spliced on the basis of isostere and mosaic theory, and a series of diarylmethylpiperazine derivatives were synthesized and their antihistaminic activities were explored. Methods The hydroxyl-substituted chromone- 2-carboxylic ester contained an aliphatic chain-linked to diarylmethylpiperazine to produce diarylmethylpiperazine derivatives. The antihistaminic activities of diarylmethylpiperazine derivatives were measured. Results The structures of diarylmethylpiperazine derivatives were identified by MS and H NMR spectra.