Pan, Bo-Wen; Shi, Yang; Li, Wen-Chao; Wang, Qing; Pan, Meng; Wu, Qiong; Fu, Hong-Zheng published the artcile< Synthesis and biological evaluation of Vinpocetine derivatives>, Application In Synthesis of 19241-24-8, the main research area is vinpocetine derivative preparation PDE1A inhibitor vasorelaxant; PDE1A; Structural modification; Vinpocetine.
A new series of Vinpocetine derivatives were synthesized and evaluated for their inhibitory activity on PDE1A in vitro. Seven compounds with higher inhibitory activity were selected for surface plasmon resonance (SPR) binding experiments Compared with Vinpocetine, these high potency compounds presented a higher binding affinity with PDE1A, which was consistent with inhibitory activity. After further screening, four compounds and Vinpocetine were selected to examine the vasorelaxant effects on endothelium-intact rat thoracic aortic rings. The study suggested that the effects of compounds I (R1 = 4-fluorophenyl) and I (R1 = 3-fluorophenyl) were the most significant with the maximum value of 93.46 ± 0.77% and 92.90 ± 0.78% (n = 5) at a concentration of 100μM resp. Based on these studies, compounds I (R1 = 4-fluorophenyl) and I (R1 = 3-fluorophenyl) were considered for further development as hit compounds
Bioorganic & Medicinal Chemistry Letters published new progress about Cerebrovascular disease. 19241-24-8 belongs to class esters-buliding-blocks, and the molecular formula is C11H13NS, Application In Synthesis of 19241-24-8.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics