Tricyclic HIV integrase inhibitors: Potent and orally bioavailable C5-aza analogs

The design and preparation of highly potent tricyclic HIV integrase inhibitors are reported. The lead compound has shown good oral bioavailability in both rat and dog. A series of C5-aza tricyclic HIV integrase inhibitors was prepared. A highly potent and orally bioavailable compound (compound 9) wa...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-02, Vol.18 (4), p.1388-1391
Main Authors: Jin, Haolun, Wright, Matthew, Pastor, Richard, Mish, Michael, Metobo, Sammy, Jabri, Salman, Lansdown, Rachael, Cai, Ruby, Pyun, Peter, Tsiang, Manuel, Chen, Xiaowu, Kim, Choung U.
Format: Article
Language:English
Subjects:
Administration, Oral
AIDS
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Azacitidine - analogs & derivatives
Azacitidine - chemistry
Azacitidine - pharmacology
Biological and medical sciences
Biological Availability
Crystallography, X-Ray
Dogs
HIV
HIV Integrase Inhibitors - chemical synthesis
HIV Integrase Inhibitors - chemistry
HIV Integrase Inhibitors - pharmacokinetics
HIV Integrase Inhibitors - pharmacology
Human immunodeficiency virus
Humans
Integrase inhibitor
Medical sciences
Organic Chemicals - chemistry
Organic Chemicals - pharmacokinetics
Organic Chemicals - pharmacology
Pharmacology. Drug treatments
Pyrrolidinones
Raltegravir Potassium
Rats
Tricyclic
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Summary:The design and preparation of highly potent tricyclic HIV integrase inhibitors are reported. The lead compound has shown good oral bioavailability in both rat and dog. A series of C5-aza tricyclic HIV integrase inhibitors was prepared. A highly potent and orally bioavailable compound (compound 9) was identified and selected for development.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.01.018