Cargando…
Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists
Twenty-one non-peptide substituted desloratadine class compounds were synthesized as novel arginine vasopressin receptor antagonists from desloratadine via successive acylation, reduction and acylation reactions. Their structures were characterized by (1)H-NMR and HRMS, their biological activity was...
Autores principales: | , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2014
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271649/ https://www.ncbi.nlm.nih.gov/pubmed/24566331 http://dx.doi.org/10.3390/molecules19022694 |
_version_ | 1783376975890481152 |
---|---|
author | Mu, Shuai Liu, Ying Gong, Min Liu, Deng-Ke Liu, Chang-Xiao |
author_facet | Mu, Shuai Liu, Ying Gong, Min Liu, Deng-Ke Liu, Chang-Xiao |
author_sort | Mu, Shuai |
collection | PubMed |
description | Twenty-one non-peptide substituted desloratadine class compounds were synthesized as novel arginine vasopressin receptor antagonists from desloratadine via successive acylation, reduction and acylation reactions. Their structures were characterized by (1)H-NMR and HRMS, their biological activity was evaluated by in vitro and in vivo studies. The in vitro binding assay and cAMP accumulation assay indicated that these compounds are potent selective V2 receptor antagonists. Among them compounds 1n, 1t and 1v exhibited both high affinity and promising selectivity for V2 receptors. The in vivo diuretic assay demonstrated that 1t presented remarkable diuretic activity. In conclusion, 1t is a potent novel AVP V2 receptor antagonist candidate. |
format | Online Article Text |
id | pubmed-6271649 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62716492018-12-20 Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists Mu, Shuai Liu, Ying Gong, Min Liu, Deng-Ke Liu, Chang-Xiao Molecules Article Twenty-one non-peptide substituted desloratadine class compounds were synthesized as novel arginine vasopressin receptor antagonists from desloratadine via successive acylation, reduction and acylation reactions. Their structures were characterized by (1)H-NMR and HRMS, their biological activity was evaluated by in vitro and in vivo studies. The in vitro binding assay and cAMP accumulation assay indicated that these compounds are potent selective V2 receptor antagonists. Among them compounds 1n, 1t and 1v exhibited both high affinity and promising selectivity for V2 receptors. The in vivo diuretic assay demonstrated that 1t presented remarkable diuretic activity. In conclusion, 1t is a potent novel AVP V2 receptor antagonist candidate. MDPI 2014-02-24 /pmc/articles/PMC6271649/ /pubmed/24566331 http://dx.doi.org/10.3390/molecules19022694 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
spellingShingle | Article Mu, Shuai Liu, Ying Gong, Min Liu, Deng-Ke Liu, Chang-Xiao Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists |
title | Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists |
title_full | Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists |
title_fullStr | Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists |
title_full_unstemmed | Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists |
title_short | Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists |
title_sort | synthesis and biological evaluation of substituted desloratadines as potent arginine vasopressin v2 receptor antagonists |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271649/ https://www.ncbi.nlm.nih.gov/pubmed/24566331 http://dx.doi.org/10.3390/molecules19022694 |
work_keys_str_mv | AT mushuai synthesisandbiologicalevaluationofsubstituteddesloratadinesaspotentargininevasopressinv2receptorantagonists AT liuying synthesisandbiologicalevaluationofsubstituteddesloratadinesaspotentargininevasopressinv2receptorantagonists AT gongmin synthesisandbiologicalevaluationofsubstituteddesloratadinesaspotentargininevasopressinv2receptorantagonists AT liudengke synthesisandbiologicalevaluationofsubstituteddesloratadinesaspotentargininevasopressinv2receptorantagonists AT liuchangxiao synthesisandbiologicalevaluationofsubstituteddesloratadinesaspotentargininevasopressinv2receptorantagonists |