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Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors
- Issue Date
- Aug-2003
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.11, no.17, pp 3589 - 3593
- Pages
- 5
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 11
- Number
- 17
- Start Page
- 3589
- End Page
- 3593
- ISSN
- 0968-0896
1464-3391
- Abstract
- 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 (IC50 = 11.8 mug/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. (C) 2003 Elsevier Ltd. All rights reserved.
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