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Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 17:5595-5599
- Publication Year :
- 2007
- Publisher :
- Elsevier BV, 2007.
-
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 CIC95 of 0.31 μM 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.
- Subjects :
- Models, Molecular
Clinical Biochemistry
Pharmaceutical Science
Integrase inhibitor
Virus Replication
Biochemistry
Cell Line
Structure-Activity Relationship
In vivo
Drug Discovery
Animals
Humans
HIV Integrase Inhibitors
Molecular Biology
chemistry.chemical_classification
Molecular Structure
biology
Organic Chemistry
HIV
Benzene
biology.organism_classification
In vitro
Rats
Integrase
Enzyme
chemistry
Viral replication
Enzyme inhibitor
Pyrazines
Lentivirus
Microsomes, Liver
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 17
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....5c7dd8e0e282073e0fa1b3f0f4f284ae
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.07.092