Synthesis of 3H-spiro[benzofuran-2,1′-cyclohexane] derivatives from naturally occurring filifolinol and their classical complement pathway inhibitory activity

Six 3H-spiro[benzofuran-2,1′-cyclohexane] derivatives were synthesized from naturally occurring filifolinol, and their classical complement pathway inhibitory activity was determined. IC50 values of the most potent compounds were comparable to the activity of the natural complement inhibitor K76-COOH and some synthetic tricyclic analogs of it.

Graphical abstractThe synthesis of six filifolinol derivatives as classical complement pathway inhibitors is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide