Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (−)-dysiherbaine

The design and synthesis of four 2,2-disubstituted dihydrobenzofurans that are structurally related to several glutamate-containing natural products, including (−)-dysiherbaine, is described. Biological evaluation of these analogs shows that one is a KA receptor antagonist and another is an NMDA receptor agonist.

The design, synthesis, and iGluR activity of a series of 2,2-disubstituted dihydrobenzofurans that are structurally related to several glutamate containing natural products, including (−)-dysiherbaine, is described.Figure optionsDownload as PowerPoint slide