Synthesis and biological evaluation of Vinpocetine derivatives was written by Pan, Bo-Wen;Shi, Yang;Li, Wen-Chao;Wang, Qing;Pan, Meng;Wu, Qiong;Fu, Hong-Zheng. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.COA of Formula: C4H7NS The following contents are mentioned in the article:
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 This study involved multiple reactions and reactants, such as Isopropylisothiocyanate (cas: 2253-73-8COA of Formula: C4H7NS).
Isopropylisothiocyanate (cas: 2253-73-8) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits, including apples, durians, pears, bananas, pineapples, and strawberries. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.COA of Formula: C4H7NS
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics