一系列5-氨基取代的4-氟苄基-8-羟基-[1,6]萘啶-7-甲酰胺HIV-1整合酶抑制剂。
A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.
作者信息
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
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jun 1;16(11):2900-4. doi: 10.1016/j.bmcl.2006.03.003. Epub 2006 Mar 22.
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.
已鉴定出一系列8-羟基[1,6]-萘啶-7-甲酰胺的5-氨基衍生物，它们在细胞培养中对HIV-1复制表现出亚微摩尔效力。其中一种类似物化合物12，在大鼠和猴子口服给药时显示出优异的药代动力学性质。该化合物被证明对感染恒河猴的猿猴-人类免疫缺陷病毒（SHIV）89.6P的复制有效。
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