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Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors |
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| Authors: | Wai John S Kim Boyoung Fisher Thorsten E Zhuang Linghang Embrey Mark W Williams Peter D Staas Donnette D Culberson Chris Lyle Terry A Vacca Joseph P Hazuda Daria J Felock Peter J Schleif William A Gabryelski Lori J Jin Lixia Chen I-Wu Ellis Joan D Mallai Rama Young Steven D |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. john_wai@merck.com |
| 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. |
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