Title of article
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors
Author/Authors
John S. Wai، نويسنده , , Boyoung Kim، نويسنده , , Thorsten E. Fisher، نويسنده , , Linghang Zhuang، نويسنده , , Mark W. Embrey، نويسنده , , Peter D. Williams، نويسنده , , Donnette D. Staas، نويسنده , , Chris Culberson، نويسنده , , Terry A. Lyle، نويسنده , , Joseph P. Vacca، نويسنده , , Daria J. Hazuda، نويسنده , , Peter J. Felock، نويسنده , , William A. Schleif، نويسنده , , Lori J. Gabryelski، نويسنده , , Lixia Jin، نويسنده , , I-Wu Chen، نويسنده , , Joan D. Ellis، نويسنده , , Rama Mallai، نويسنده , , Steven D. Young، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
5595
To page
5599
Abstract
A series of potent novel dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 6 is active against replication of HIV with a CIC95 of 0.31 μM and exhibits no shift in potency in the presence of 50% normal human serum. It displays a good pharmacokinetic profile when dosed in rats and no covalent binding with microsomal proteins in both in vitro and in vivo models.
Keywords
HIV , integrase , Strand transfer inhibitors , 6-dione , Dihydroxypyridopyrazine-1
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798661
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