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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors.

HIV-1 integrase (IN) is an essential enzyme for retroviral replication and a rational target for the design of anti-AIDS drugs. In the present study, we have designed, synthesized and tested a series of caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors. Among these compounds, we found that HIV integrase inhibitory activities of compounds III-3 and III-4 were more potent than L-chicoric acid (IC(50)=11.8 microg/mL) and others were comparable to L-chicoric acid. Furthermore, the structure-activity relationships of these compounds were studied. The information gathered from this paper will be useful in the development and design of HIV-1 integrase inhibitors in the future.[1]


  1. Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors. Xu, Y.W., Zhao, G.S., Shin, C.G., Zang, H.C., Lee, C.K., Lee, Y.S. Bioorg. Med. Chem. (2003) [Pubmed]
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