Abstract：OBJECTIVE To design and synthesize a series of novel V2 receptor antagonists according to the drug structure-activity relationship in order to screen out compounds with high efficacy and low toxicity and create conditions for preclinical research and lay foundation for the development of new drugs. METHODS A number of novel V2 receptor antagonists were synthesized according to the design idea of “me-too”. The structure was confirmed by 1H-NMR and HRMS, and the physicochemical constants related to the melting point and purity were determined. Biological activity was evaluated by cell model expressing human V2 receptor and rat diuretic model. RESULTS Twelve novel structural compounds(A1-A12) were designed and synthesized, among which A6, A7, A11 and other compounds showed strong biological activity and a longer duration of action than the existing V2 receptor antagonists. CONCLUSION The reasonable structure design of the compound has certain reference value for the further research on the structure modification of V2 receptor antagonist and their pharmacological and toxicological activities.
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2022, Vol. 57 
