Author/Authors :
William J. Hornback، نويسنده , , John E. Munroe، نويسنده , , Timothy A. Shepherd، نويسنده , , Steve D. Hatch، نويسنده , , Mark A. Muesing، نويسنده , , MaryAnn Wiskerchen، نويسنده , , Joseph M. Colacino، نويسنده , , Angela J. Baxter، نويسنده , , Kenneth S. Su، نويسنده , , Kristina M. Campanale، نويسنده ,
Abstract :
Using the hydroxyethylamine isosteres 1 and 2 containing the novel cis-octahydrothienopyridine moiety, substantial enhancement of binding potencies for HIV-1 protease inhibitors which incorporate carbamate linked heterocyclic P2 ligands has been realized. This increase in binding has led to a very potent antiviral compound (LY326188). The pharmacokinetics of selected derivatives are detailed in this report.