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A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors |
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| Authors: | Guare James P Wai John S Gomez Robert P Anthony Neville J Jolly Samson M Cortes Amanda R Vacca Joseph P Felock Peter J Stillmock Kara A Schleif William A Moyer Gregory Gabryelski Lori J Jin Lixia Chen I-Wu Hazuda Daria J Young Steven D |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. jim_guare@merck.com |
| Abstract: | A series of 5-amino derivatives of 8-hydroxy1,6]-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. |
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