Title of article
A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors
Author/Authors
James P. Guare، نويسنده , , John S. Wai، نويسنده , , Robert P. Gomez، نويسنده , , Neville J. Anthony، نويسنده , , Samson M. Jolly، نويسنده , , Amanda R. Cortes، نويسنده , , Joseph P. Vacca، نويسنده , , Peter J. Felock، نويسنده , , Kara A. Stillmock، نويسنده , , William A. Schleif، نويسنده , , Gregory Moyer، نويسنده , , Lori J. Gabryelski، نويسنده , , Lixia Jin، نويسنده , , I-Wu Chen، نويسنده , , Daria J. Hazuda، نويسنده , , Steven D. Young، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
2900
To page
2904
Abstract
A series of 5-amino derivatives of 8-hydroxy[1,6]-naphthyridine-7-carboxamide exhibiting sub-micromolar potency against replication of HIV-1 in cell culture was identified. One of these analogs, compound 12, displayed excellent pharmacokinetic properties when dosed orally in rats and in monkeys. This compound was demonstrated to be efficacious against replication of simian-human immunodeficiency virus (SHIV) 89.6P in infected rhesus macaques.
Keywords
HIV-1 , integrase , inhibitor , monkey , rhesus , macaque , Naphthyridine
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796893
Link To Document