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

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

Received: 2 December 2013; in revised form: 14 January 2014 / Accepted: 26 January 2014 / Published: 24 February 2014
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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.
Keywords: substituted desloratadine; synthesis; arginine vasopressin receptor antagonists; biological activity
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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.

AMA 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(2):2694-2706.

Chicago/Turabian Style

Mu, Shuai; Liu, Ying; Gong, Min; Liu, Deng-Ke; Liu, Chang-Xiao. 2014. "Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists." Molecules 19, no. 2: 2694-2706.

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