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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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-02, Vol.18 (4), p.1388-1391
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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