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Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors

Authors :
Joseph P. Vacca
Linghang Zhuang
Lori J. Gabryelski
Terry A. Lyle
William A. Schleif
Peter J. Felock
Boyoung Kim
Lixia Jin
I.-W. Chen
Donnette D. Staas
Chris Culberson
Steven D. Young
Daria J. Hazuda
Thorsten E. Fisher
John S. Wai
Peter D. Williams
Mark Embrey
Rama Mallai
Joan D. Ellis
Source :
Bioorganic & Medicinal Chemistry Letters. 17:5595-5599
Publication Year :
2007
Publisher :
Elsevier BV, 2007.

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.

Details

ISSN :
0960894X
Volume :
17
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....5c7dd8e0e282073e0fa1b3f0f4f284ae
Full Text :
https://doi.org/10.1016/j.bmcl.2007.07.092