Design and synthesis of dual active neovibsanin derivatives based on a chemical structure merging method.

Basic Information

ID: ALA4665757

Journal: Bioorg Med Chem Lett

Title: Design and synthesis of dual active neovibsanin derivatives based on a chemical structure merging method.

Authors: Yanagimoto T,Kishimoto S,Kasai Y,Matsui N,Kubo M,Yamamoto H,Fukuyama Y,Imagawa H

Abstract: A hybrid compound consisting of neovibsanin and trans-banglene was designed according to a structure merging method and synthesized via a sequence of key steps including a Diels-Alder cycloaddition, stereoselective alkynylation, and intramolecular oxa-Michael addition reaction. The biological activity of the synthetized acetal compound and its hemiacetal analogue was investigated in PC12 cells. These studies revealed that the designed hybrid compounds displayed neuritogenic activity. Furthermore, a relatively strong neurite outgrowth promoting activity was observed in the presence of NGF. These results suggest that the designed hybrid compound exhibited a dual activity.

CiteXplore: 32800919

DOI: 10.1016/j.bmcl.2020.127497

Patent ID: