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Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity |
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| Authors: | Bénard Christophe Zouhiri Fatima Normand-Bayle Marie Danet Michèle Desmaële Didier Leh Hervé Mouscadet Jean-François Mbemba Gladys Thomas Claire-Marie Bonnenfant Sabine Le Bret Marc d'Angelo Jean |
| Institution: | CNRS UMR 8076, Centre d'Etudes Pharmaceutiques, Chimie Organique, 5 rue J.-B. Clément, 92296 Chatenay-Malabry, France. |
| Abstract: | A novel series of HIV-1 integrase inhibitors was synthesized and tested in both in vitro and ex vivo assays. These inhibitors are featured by the presence of a quinoline subunit and an ancillary aromatic ring linked by functionalized spacers such as amide, hydrazide, urea and 1-hydroxyprop-1-en-3-one moiety. Amide derivatives are the most promising ones and could serve as leads for further developments. |
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