Author/Authors :
Michel Evers، نويسنده , , Jean-Claude Barrière، نويسنده , , Georges Bashiardes، نويسنده , , Anne Bousseau، نويسنده , , Jean-Christophe Carry، نويسنده , , Norbert Dereu، نويسنده , , Bruno Filoche، نويسنده , , Yvette Henin، نويسنده , , Serge Sablé، نويسنده , , Marc Vuilhorgne، نويسنده , , Serge Mignani، نويسنده ,
Abstract :
Original cyclosporin A (CsA) derivatives bearing various alkylthio side chains at the sarcosine residue 3 (R configuration) and for the most potent and selective compounds a 4′-hydroxyl group at the Me-Leucine residue 4 were prepared in one or two steps from commercially available CsA. The [2-(dimethyl or diethylamino)-ethylthio-Sar]3-[(4′-OH)MeLeu]4-CsA derivatives 3k and 3l displayed potent in vitro anti-HIV-1 (IC50 46 nM) and low immunosuppressive activities (IC50≥1500 nM).
