Synthesis and evaluation of 3′-azido-2′,3′-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:20

Article

Zhang, Hong-wang^1,2  Coats, Steven J.³  Bondada, Lavanya^1,2  Amblard, Franck^1,2  Detorio, Mervi^1,2  Asif, Ghazia^1,2  Fromentin, Emilie^1,2  Solomon, Sarah^1,2  Obikhod, Aleksandr^1,2  Whitaker, Tony³  Sluis-Cremer, Nicolas⁴  Mellors, John W.⁴  Schinazi, Raymond F.^1,2 

[1] Emory Univ, Sch Med, Dept Pediat, Ctr AIDS Res,Lab Biochem Pharmacol, Atlanta, GA 30033 USA

[2] Vet Affairs Med Ctr, Atlanta, GA 30033 USA

[3] RFS Pharma LLC, Tucker, GA 30084 USA

[4] Univ Pittsburgh, Sch Med, Div Infect Dis, Dept Med, Pittsburgh, PA 15261 USA

关键词: HIV-1;    Nucleoside;    Antiviral;    Transglycosylation;   

DOI  :  10.1016/j.bmcl.2009.11.031

来源: Elsevier

【 摘 要 】

Based on the promising drug resistance profile and potent anti-HIV activity of beta-D-3'-azido-2',3'-dideoxyguanosine, a series of purine modified nucleosides were synthesized by a chemical transglycosylation reaction and evaluated for their antiviral activity, cytotoxicity, and intracellular metabolism. Among the synthesized compounds, several show potent and selective anti-HIV activity in primary lymphocytes. Published by Elsevier Ltd.

【 授权许可】

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