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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Embrey, M.W. et al.

Embrey, Wai, Funk, Homnick, Perlow, Young, Vacca, Hazuda, Felock, Stillmock, Witmer, Moyer, Schleif, Gabryelski, Jin, Chen, Ellis, Wong, Lin, Leonard, Tsou, Zhuang,

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.

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.[1]

References

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. Embrey, M.W., Wai, J.S., Funk, T.W., Homnick, C.F., Perlow, D.S., Young, S.D., Vacca, J.P., Hazuda, D.J., Felock, P.J., Stillmock, K.A., Witmer, M.V., Moyer, G., Schleif, W.A., Gabryelski, L.J., Jin, L., Chen, I.W., Ellis, J.D., Wong, B.K., Lin, J.H., Leonard, Y.M., Tsou, N.N., Zhuang, L. Bioorg. Med. Chem. Lett. (2005) [Pubmed]

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