| Literature DB >> 17822898 |
John S Wai1, Boyoung Kim, Thorsten E Fisher, Linghang Zhuang, Mark W Embrey, Peter D Williams, Donnette D Staas, Chris Culberson, Terry A Lyle, Joseph P Vacca, Daria J Hazuda, Peter J Felock, William A Schleif, Lori J Gabryelski, Lixia Jin, I-Wu Chen, Joan D Ellis, Rama Mallai, Steven D Young.
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 CIC(95) of 0.31 microM 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.Entities:
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Year: 2007 PMID： 17822898 DOI： 10.1016/j.bmcl.2007.07.092
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823