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

Basic Information

ID: ALA1146726

Journal: Bioorg Med Chem Lett

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

Authors: Bénard C, Zouhiri F, Normand-Bayle M, Danet M, Desmaële D, Leh H, Mouscadet JF, Mbemba G, Thomas CM, Bonnenfant S, Le Bret M, d'Angelo J.

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.

CiteXplore: 15109635

DOI: 10.1016/j.bmcl.2004.03.005

Patent ID: