Synthesis and biological evaluation of novel derivatives of desloratadine

被引：3

作者：

Mu, Shuai ^{[1
,2
]}

Xie, Xiao-Shuai ^{[3
]}

Niu, Duan ^{[3
]}

Zhang, Da-Shuai ^{[3
]}

Liu, Deng-Ke ^{[4
]}

Liu, Chang-Xiao ^{[2
]}

机构：

[1] Tianjin Univ, Sch Chem Engn & Technol, Tianjin 300072, Peoples R China

[2] Tianjin Inst Pharmaceut Res, State Key Lab Drug Delivery Technol & Pharmacokin, Tianjin 300193, Peoples R China

[3] Tianjin Med Univ, Grad Sch, Tianjin 300070, Peoples R China

[4] Tianjin Inst Pharmaceut Res, Tianjin Key Lab Mol Design & Drug Discovery, Tianjin 300193, Peoples R China

来源：

CHINESE CHEMICAL LETTERS | 2013年 / 24卷 / 06期

关键词：

Derivatives of desloratadine; Arginine vasopressin receptor antagonists; Diuretic activity; VASOPRESSIN ANTAGONISTS;

D O I：

10.1016/j.cclet.2013.03.041

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Series of novel derivatives of desloratadine designed as arginine vasopressin receptor antagonists were synthesized and structurally characterized by melting points, H-1 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 Via receptor. Our studies indicated that desloratadine may be an active substructure for novel arginine vasopressin receptor antagonist development. (C) 2013 Chang-Xiao Liu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

引用

页码：531 / 534

页数：4

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