GERANYL DERIVATIVES OF SALSOLINOL SHOW INCREASED BIOLOGICAL ACTIVITIES

Salsolinol and its N- and N,N-geranylated derivatives were tested for antimicrobial, cytotoxic, anti-oxidant, and anti-HIV activities, as well as inhibitory activity against Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. N,N-Geranylation increased potency in three different assays, antimicrobial, cytotoxic, and EBV-EA, while N-geranylation increased potency to a lesser extent in these same assays. N,N-Geranylated salsolinol was significantly active in all assays, except anti-HIV, and may be useful as a lead compound for developing potential chemotherapeutic agents.