Author/Authors :
Edmund L. Ellsworth، نويسنده , , John Domagala، نويسنده , , J. V. N. Vara Prasad، نويسنده , , Susan Hagen، نويسنده , , Donna Ferguson، نويسنده , , Tod Holler، نويسنده , , Donald Hupe، نويسنده , , Neil Graham، نويسنده , , Caroline Nouhan، نويسنده , , Peter J. Tummino، نويسنده , , Greg Zeikus، نويسنده , , Elizabeth A. Lunney، نويسنده ,
Abstract :
5,6-Dihydro-2H-pyran-2-ones are potent inhibitors of HIV-1 protease, which bind to the S1, S2, S1′, and S2′ pockets and have a unique binding mode with the catalytic aspartyl groups and the flap region of the enzyme. Efforts to explore 3-position heterocyclic scaffolds that bind to the S1′ and S2′ pockets have provided a number of selected analogs that display high HIV-1 protease inhibitory activity.
