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本文作者合成了新的５，７二甲基１，２，４三唑并［１，５ａ］嘧啶２苄硫醚类（Ｂ系列）５，７二甲基１，２，４三唑并［３，４ａ］嘧啶２苄硫醚类化合物（Ｄ系列），并测定了这两类化合物在体外对８５７ｍｍｏｌ·Ｌ１Ｋ＋和１０４ｍｍｏｌ·Ｌ１ＮＥ（ｎｏｒｅｐｉｎｅｐｈｒｉｎｅ）引起的血管条收缩的抑制作用。测定结果表明，Ｂ系列化合物的活性均高于Ｄ系列化合物，在苯环的对位有体积较大的疏水性基团有助于生物活性的提高。５，７二甲基１，２，４三唑并［１，５ａ］嘧啶２对溴苄硫醚表现出最好的扩张血管活性，在浓度为１０５ｍｏｌ·Ｌ１和１０４ｍｏｌ·Ｌ１时，对１０４ｍｍｏｌ·Ｌ１ＮＥ引起的离体血管条痉挛的抑制率均为１００％；对８５７ｍｍｏｌ·Ｌ１Ｋ＋引起的离体血管条痉挛的抑制率分别为４７％和１００％。
The authors synthesized a new 5,7 dimethyl 1, 2,4 triazolo [1,5a] pyrimidine 2 benzyl sulfide (B series) 5,7 dimethyl 1,2,4 triazolo [3,4 a] pyrimidine 2 benzyl sulfide compounds (D series), and the determination of these two compounds in vitro 85 7mmol·L 1K + and 10 4mmol · L 1NE (nor epinephrine) caused by inhibition of vascular contraction. The results showed that the activity of B series compounds was higher than that of D series compounds, and the larger hydrophobic groups in the para position of benzene ring contributed to the increase of biological activity. 5,7 dimethyl 1,2,4 triazolo [1,5a] pyrimidine 2 bromobenzyl ether showed the best vasodilator activity in the concentration of 10 5mol·L 1 and 10 4mol·L 1, 10 4mmol·L 1NE caused by inhibition of isolated vascular spasm were 100%; on 85 7mmol L 1K + isolated vascular spasm The inhibition rate was 47% and 100% respectively.