Ali F E, Gleason J G, Hill D T, Krell R D, Kruse C H, Lavanchy P G, Volpe B W
J Med Chem. 1982 Oct;25(10):1235-40. doi: 10.1021/jm00352a028.
As part of a study of the influence of structural modifications of N',N'-bis(aralkyl)imidodisulfamides on their ability to selectively antagonize SRS-A activity, a few conformationally constrained structures were examined. Among these derivatives having a conformationally restricted alkylene side chain, substituted 1,2,3,4-tetrahydroisoquinolinylsulfonic imides produced optimum SRS-A antagonist activity and selectivity. These compounds were tested for antagonism of partially purified SRS-A induced contractions of isolated guinea pig ileum. In this series of tetrahydroisoquinolines, the effect of aromatic ring substitution, as well as substitution and variation of the size of the heterocyclic ring on SRS-A antagonist activity and selectivity, was studied.
作为一项关于N',N'-双(芳烷基)亚氨基二硫酰胺结构修饰对其选择性拮抗SRS-A活性能力影响的研究的一部分,研究了一些构象受限的结构。在这些具有构象受限亚烷基侧链的衍生物中,取代的1,2,3,4-四氢异喹啉基磺酸酰亚胺产生了最佳的SRS-A拮抗活性和选择性。测试了这些化合物对部分纯化的SRS-A诱导的离体豚鼠回肠收缩的拮抗作用。在这一系列四氢异喹啉中,研究了芳环取代以及杂环大小的取代和变化对SRS-A拮抗活性和选择性的影响。