Beattie D E, Crossley R, Curran A C, Hill D G, Lawrence A E
J Med Chem. 1977 May;20(5):718-21. doi: 10.1021/jm00215a020.
A series of thioureas derived from 5,6,7,8-tetrahydroquinoline, 1,5-, 1,6-, and 1,8-naphthyridiness, pyrido[2,3-b]azepine, and 7-azaindoline has been prepared and tested for antisecretory activity in the pylorus-ligated rat and protective activity against gastric erosions caused by cold-restraint stress. The thioureas exhibit different structure-activity relationships from the corresponding 5,6,7,8-tetrahydroquinoline-8-thiocarboxamides and these relationships are discussed. The activity of the thioureas is less affected by structural differences than the corresponding thioamides although they probably have the same mode of action.
已经制备了一系列衍生自5,6,7,8-四氢喹啉、1,5-、1,6-和1,8-萘啶、吡啶并[2,3 - b]氮杂䓬和7-氮杂吲哚的硫脲，并在幽门结扎大鼠中测试了其抗分泌活性以及对冷束缚应激引起的胃糜烂的保护活性。这些硫脲与相应的5,6,7,8-四氢喹啉-8-硫代羧酰胺表现出不同的构效关系，并对这些关系进行了讨论。尽管硫脲和相应的硫代酰胺可能具有相同的作用模式，但硫脲的活性受结构差异的影响比相应的硫代酰胺小。
