Article
10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants.
Bioorganic & medicinal chemistry letters - 15 Aug 2008
Wiscount Catherine M, Williams Peter D, Tran Lekhanh O, Embrey Mark W, Fisher Thorsten E, Sherman Vanessa, Homnick Carl F, Donnette Staas D, Lyle Terry A, Wai John S, Vacca Joseph P, Wang ZiQiang, Felock Peter J, Stillmock Kara A, Witmer Marc V, Miller Michael D, Hazuda Daria J, Day Alysha M, Gabryelski Lori J, Ecto Linda T, Schleif William A, DiStefano Daniel J, Kochansky Christopher J, Anari M Reza
Abstract excerpt
A series of 10-hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones was synthesized and tested for their inhibition of HIV-1 replication in cell culture. Structure-activity studies indicated that high antiviral potency against wild-type virus as well as viruses containing integrase mutations that confer resistance to three different structural classes of integrase inhibitors could be...
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