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. 2004 May 17;14(10):2473-6.
doi: 10.1016/j.bmcl.2004.03.005.

Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity

Christophe Bénard  1 , Fatima Zouhiri, Marie Normand-Bayle, Michèle Danet, Didier Desmaële, Hervé Leh, Jean-François Mouscadet, Gladys Mbemba, Claire-Marie Thomas, Sabine Bonnenfant, Marc Le Bret, Jean d'Angelo
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Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity

Christophe Bénard et al. Bioorg Med Chem Lett. .

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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