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. 2005 Oct 15;15(20):4550-4.
doi: 10.1016/j.bmcl.2005.06.105.

A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells

Mark W Embrey  1 , 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
Affiliations

A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells

Mark W Embrey et al. Bioorg Med Chem Lett. .

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.

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