Newly Synthesized Fluorinated Cinnamylpiperazines Possessing Low In Vitro MAO-B Binding.

ABSTRACT: Herein, we report on the synthesis and pharmacological evaluation of ten novel fluorinated cinnamylpiperazines as potential monoamine oxidase B (MAO-B) ligands. The designed derivatives consist of either cinnamyl or 2-fluorocinnamyl moieties connected to 2-fluoropyridylpiperazines. The three-step synthesis starting from commercially available piperazine afforded the final products in overall yields between 9% and 29%. An in vitro competitive binding assay using l-[³H]Deprenyl as radioligand was developed and the MAO-B binding affinities of the synthesized derivatives were assessed. Docking studies revealed that the compounds 8-17 were stabilized in both MAO-B entrance and substrate cavities, thus resembling the binding pose of l-Deprenyl. Although our results revea

SUBMITTER: I Jevtic I 

PROVIDER: S-EPMC7663645 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature