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本文设计、合成了一系列咳嗽衍生物（Ⅰ－Ⅱ），并检测了它们的血管紧张素Ⅱ受体拮机活性。以ZD-731（pA2＝84）为先导化合物，用生物电子等排的N－苯基吡咯羧酸、N－苯基吡咯四氮唑和苯氧基苯乙酸代替ZD－8731的联苯四氮哇获得化合物（Ⅰ）、（Ⅱ）和（Ⅲ）。结果这些结构变化有损于活性。在离体试验中（兔胸主动脉坏），所有的化合物均显示了竞争性拮抗活性。这三类化合物的活性最高者分别为（Id）（pA2值为6．8），（Ⅱa）（pA2值为77）和（Ⅲc）（pA2值为77），活性分别比ZD－8731低40、5和12倍。本文并对它们的构效关系和构象比较进行了讨论。
In this paper, we designed and synthesized a series of cough derivatives (Ⅰ-Ⅱ) and tested their angiotensin Ⅱ receptor antagonistic activity. ZD-731 (pA2 = 84) was used as the lead compound and bioelectrical isosorbide N-phenylpyrrole carboxylic acid, N-phenylpyrrole tetrazolium and phenoxyphenylacetic acid were used instead of biphenyltetrazolium Wow to obtain compounds (I), (II) and (III). As a result, these structural changes detract from activity. In an in vitro study (rabbit thoracic aorta bad), all of the compounds showed competitive antagonistic activity. The activities of these three compounds were (Id) (pA2 = 6.8), (Ⅱa) (pA2 = 77) and (Ⅲc) (pA2 = 77) , 5 and 12 times. This article also discusses their structure-activity relationship and conformational comparison.