Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester

A series of nitrogen-containing polyhydroxylated aromatics from caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase inhibitors. Most of these compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in the 3′-end processing and the strand transfer. Their key structure–activity relationship was also discussed.

Graphical abstractA series of novel nitrogen-containing polyhydroxylated aromatics were evaluated for their ability to inhibit HIV-1 integrase at micromolar concentrations.Figure optionsDownload full-size imageDownload as PowerPoint slide