Imidodisulfamides. 2. Substituted 1,2,3,4-tetrahydroisoquinolinylsulfonic imides as antagonists of slow-reacting substance of anaphylaxis.
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.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D007094:Imides / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D013189:SRS-A / Q000037:antagonists & inhibitors*
D007094:Imides; D007546:Isoquinolines; D013189:SRS-A