Synthesis and Activity Evaluation of Vinpocetine-Derived Indole Alkaloids.

ABSTRACT: This study focuses on the synthesis of novel vinpocetine derivatives (2-25) and their biological evaluation. The chemical structures of the synthesized compounds were fully characterized using techniques such as ¹H NMR, ¹³C NMR, and HRMS. The inhibitory activity of the synthesized compounds on PDE1A was evaluated, and the results revealed that compounds 3, 4, 5, 12, 14, 21, and 25 exhibited superior inhibitory activity compared to vinpocetine. Compound 4, with a para-methylphenyl substitution, showed a 5-fold improvement in inhibitory activity with an IC₅₀ value of 3.53 ± 0.25 μM. Additionally, compound 25, with 3-chlorothiazole substitution, displayed an 8-fold increase in inhibit

SUBMITTER: Dong ZC 

PROVIDER: S-EPMC10779641 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature