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

C Bénard, F Zouhiri, M Normand-Bayle, M Danet…

Index: Benard, Christophe; Zouhiri, Fatima; Normand-Bayle, Marie; Danet, Michele; Desmaele, Didier; Leh, Herve; Mouscadet, Jean-Francois; Mbemba, Gladys; Thomas, Claire-Marie; Bonnenfant, Sabine; Le Bret, Marc; D'Angelo, Jean Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 10 p. 2473 - 2476

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Citation Number: 94

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.