Author/Authors :
John E. Munroe، نويسنده , , William J. Hornback، نويسنده , , Jack B. Campbell، نويسنده , , Michael A. Ouellette، نويسنده , , Steve D. Hatch، نويسنده , , Mark A. Muesing، نويسنده , , Mary Ann Wiskerchen، نويسنده , , Angela J. Baxter، نويسنده , , Ken Su، نويسنده , , Kristina Campanale، نويسنده ,
Abstract :
Replacement of the decahydroisoquinoline group contained in Ro 31-8959 by a cis-octahydrothienopyridine moiety has provided a high affinity hydroxyethylamine isostere for use in HIV-1 protease inhibitors. Further gains in potency have been realized by incorporation of a sulfur atom into the P1 benzyl group. Modification by a key P2 ligand provided LY316440, a potent, orally absorbed inhibitor of HIV-1 protease.
