Citation: Shuang Zhi, Shuai Mu, Ying Liu, Min Gong, Ping-Bao Wang, Deng-Ke Liu. Synthesis and biological evaluation of novel phenothiazine derivatives as non-peptide arginine vasopressin V2 receptor antagonists[J]. Chinese Chemical Letters, ;2015, 26(5): 627-630. doi: 10.1016/j.cclet.2015.01.022 shu

Synthesis and biological evaluation of novel phenothiazine derivatives as non-peptide arginine vasopressin V2 receptor antagonists

Shuang Zhi ^a ,
Shuai Mu ^a,b ,
Ying Liu ^b ,
Min Gong ^b ,
Ping-Bao Wang ^b ,
Deng-Ke Liu ^b,,

1.
a School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China;
2.
b Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China

Corresponding author: Deng-Ke Liu,
Received Date: 27 January 2014
Available Online: 23 December 2014
Fund Project:

A series of novel phenothiazine derivatives was synthesized and tested for arginine vasopressin receptor antagonist activity. They were synthesized as novel arginine vasopressin receptor antagonists from phenothiazine as a scaffold via successive acylation, reduction and acylation reactions. Their structures were characterized by ¹HNMR, ¹³CNMRandHRMS, and biological activitywas evaluated by in vitro and in vivo studies. The in vitro binding assay indicated that several compounds are potent selective V2 receptor antagonists. Compounds with promising binding affinity to V2 receptors were selected to conduct the in vivo diuretic studies on Sprague-Dawley rats. Among them, 1n, 1r, 1t and 1v exhibited excellent diuretic activity, especially 1r and 1v. Therefore, 1r and 1v are potent novelAVP V2receptor antagonist candidates.
- Arginine vasopressin V2 receptor,
- antagonist,
- Phenothiazine derivatives,
- Synthesis,
- Biological activities
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