| Literature DB >> 16102965 |
Mark W Embrey1, John S Wai, Timothy W Funk, Carl F Homnick, Debbie S Perlow, Steven D Young, Joseph P Vacca, Daria J Hazuda, Peter J Felock, Kara A Stillmock, Marc V Witmer, Gregory Moyer, William A Schleif, Lori J Gabryelski, Lixia Jin, I-Wu Chen, Joan D Ellis, Bradley K Wong, Jiunn H Lin, Yvonne M Leonard, Nancy N Tsou, Linghang Zhuang.
Abstract
Introduction of a 5,6-dihydrouracil functionality in the 5-position of N-(4-fluorobenzyl)-8-hydroxy-[1,6]naphthyridine-7-carboxamide 1 led to a series of highly active HIV-1 integrase inhibitors. These compounds displayed low nanomolar activity in inhibiting both the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 11 is a 150-fold more potent antiviral agent than 1, with a CIC(95) of 40 nM in the presence of human serum. It displays good pharmacokinetics when dosed in rats and dogs.Entities:
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Year: 2005 PMID： 16102965 DOI： 10.1016/j.bmcl.2005.06.105
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823