Next Article in Journal
Acknowledgement to Reviewers of Molecules in 2013
Previous Article in Journal
Characteristics, Composition and Oxidative Stability of Lannea microcarpa Seed and Seed Oil
Article Menu

Export Article

Open AccessArticle
Molecules 2014, 19(2), 2694-2706; doi:10.3390/molecules19022694

Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists

1
School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China
2
Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
3
State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
*
Author to whom correspondence should be addressed.
Received: 2 December 2013 / Revised: 14 January 2014 / Accepted: 26 January 2014 / Published: 24 February 2014
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [268 KB, uploaded 18 June 2014]   |  

Abstract

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 1H-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. View Full-Text
Keywords: substituted desloratadine; synthesis; arginine vasopressin receptor antagonists; biological activity substituted desloratadine; synthesis; arginine vasopressin receptor antagonists; biological activity
Figures

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Mu, S.; Liu, Y.; Gong, M.; Liu, D.-K.; Liu, C.-X. Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists. Molecules 2014, 19, 2694-2706.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top