Synthesis and biological evaluation of novel derivatives of desloratadine

Abstract Series of novel derivatives of desloratadine designed as arginine vasopressin receptor antagonists were synthesized and structurally characterized by melting points, 1 H 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.