组胺H_2受体拮抗剂的研究——胍基噻唑衍生物的合成

STUDIES ON HISTAMINE H_2 RECEPTOR ANTAGONIST—SYNTHESIS OF GUANITHIAZOLE DERIVATIVES

本文根据H_2受体拮抗剂作用原理及药物体内吸收、代谢规律,设计并合成了九个结构类似的胍基噻唑类化合物,经实步药理实验表明,化合物C-173和C-174对组胺H_2受体的拮抗作用较强,有必要进一步研究。

Nine guanithiazole derivatives were synthesized and were evaluated in their antisecretory activity in vitro. Two of them (the compounds C-173 and C-174) have more potent antisecretoy activity than cimetidine possibly, and eight of them are new compounds. A further study is necessary.