Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity
作者:Christophe Bénard、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
DOI:10.1016/j.bmcl.2004.03.005
日期:2004.5
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-l-en-3-one moiety. Amide derivatives are the most promising ones and could serve as leads for further developments. (C) 2004 Elsevier Ltd. All rights reserved.