Synthesis and biological evaluation of novel derivatives of desloratadine  

作　　者：Shuai Mu Xiao-Shuai Xie Duan Niu Da-Shuai Zhang Deng-Ke Liu Chang-Xiao Liu 

机构地区：[1]School of Chemical Engineering and Technology,Tianjin University [2]State Key Laboratory of Drug Delivery Technology and Pharmacokinetics,Tianjin Institute of Pharmaceutical Research [3]Graduate School of Tianjin Medical University [4]Tianjin Key Laboratory of Molecular Design and Drug Discovery,Tianjin Institute of Pharmaceutical Research

出　　处：《Chinese Chemical Letters》2013年第6期531-534,共4页中国化学快报（英文版）

基　　金：project was supported by National 973 Plan(Nos. 2010CB735602 and 2012CB724002);National Major Scientific and Technological Special Project for "Significant New Drugs Development"(No.2011ZX09401-009)

摘　　要：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 VI a receptor.Our studies indicated that desloratadine may be an active substructure for novel arginine vasopressin receptor antagonist development.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 VI a receptor.Our studies indicated that desloratadine may be an active substructure for novel arginine vasopressin receptor antagonist development.

关 键 词：Derivatives of desloratadine Arginine vasopressin receptor antagonists Diuretic activity 

分 类 号：R575.2[医药卫生—消化系统]