1423771-99-6Relevant articles and documents
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
, p. 2694 - 2706 (2014)
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.
Synthesis and biological evaluation of novel derivatives of desloratadine
Mu, Shuai,Xie, Xiao-Shuai,Niu, Duan,Zhang, Da-Shuai,Liu, Deng-Ke,Liu, Chang-Xiao
, p. 531 - 534 (2013/07/27)
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