Synthesis and biological evaluation of novel derivatives of desloratadine

Series of novel derivatives of desloratadine designed as arginine vasopressin receptor antagonists were synthesized and structurally characterized by melting points, 1H NMR and HRMS. Their in vivo diuretic activities were evaluated on rats, and several target compounds showed promising diuretic results, especially compounds 8, 18, 27 and 31. Further in vitro bonding assay and cAMP assay showed that these compounds had a higher affinity to vasopressin V2 receptor than V1a receptor. Our studies indicated that desloratadine may be an active substructure for novel arginine vasopressin receptor antagonist development.

Twenty-nine derivatives of desloratadine were synthesized and evaluated. Several compounds showed promising diuretic activity.Figure optionsDownload as PowerPoint slide