Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors
| Autor: | Cha-Gyun Shin, Chong-Kyo Lee, Heng-Chang Zang, Guisen Zhao, Yu-Wen Xu, Yong Sup Lee |
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| Rok vydání: | 2003 |
| Předmět: |
Anti-HIV Agents
medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Integrase inhibitor Carboxamide HIV Integrase Biochemistry Chemical synthesis Drug Discovery medicine HIV Integrase Inhibitors Molecular Biology chemistry.chemical_classification Sulfonamides biology Chemistry Organic Chemistry biology.organism_classification Integrase Enzyme Viral replication Enzyme inhibitor Lentivirus biology.protein Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry. 11:3589-3593 |
| ISSN: | 0968-0896 |
| Popis: | 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 μg/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. |
| Databáze: | OpenAIRE |
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