Acid-stable 2'-fluoro purine dideoxynucleosides as active agents against HIV

…, JS Roth, S Broder, DG Johns, JS Driscoll

文献索引：Marquez; Tseng; Mitsuya; Aoki; Kelley; Ford Jr.; Roth; Broder; Johns; Driscoll Journal of Medicinal Chemistry, 1990 ,  vol. 33,  # 3  p. 978 - 985

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被引用次数: 230

摘要

2', 3'-Dideoxy purine nucleosides have anti-HIV activity in vitro and the inosine analogue is being clinically evaluated. The instability of these compounds toward acidic conditions complicates oral administration. The effect of the addition of a fluorine atom to the 2'-position was investigated by preparing the fluorine-containing 2'-erythro and 2'-threo isomers of ddA and the threo isomer of ddI. All fluorine-containing compounds were indefinitely stable to ...