Author/Authors :
Thorsten E. Fisher، نويسنده , , Boyoung Kim، نويسنده , , Donnette D. Staas، نويسنده , , Terry A. Lyle، نويسنده , , Steven D. Young، نويسنده , , Joseph P. Vacca، نويسنده , , Matthew M. Zrada، نويسنده , , Daria J. Hazuda، نويسنده , , Peter J. Felock، نويسنده , , William A. Schleif، نويسنده , , Lori J. Gabryelski، نويسنده , , M. Reza Anari، نويسنده , , Christopher J. Kochansky، نويسنده , , John S. Wai، نويسنده ,
Abstract :
A series of potent novel 8-hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 12 is active against replication of HIV-1 in cell culture with a CIC95 of 0.31 μM. Further SAR exploration led to the preparation of pseudosymmetrical tricyclic pyrrolopyrazine inhibitors 23 and 24 with further improvement in antiviral activity.
