Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan®

Small molecule agonists and antagonists of the V2-vasopressin receptor have been discovered and have undergone clinical trials. In conjunction with these discovery programs, the synthesis and biological testing of various metabolites associated with these clinical targets were actively pursued. We now report the results of our synthetic efforts and the corresponding biological data generated for several of the metabolites of WAY-151932 and CL-347985 (Lixivaptan®).

Graphical abstractThe synthesis and biological results for metabolites of the above vasopressin agonist 1 and antagonist 2 are presented.Figure optionsDownload full-size imageDownload as PowerPoint slide