- Synthesis and evaluation of 3′-azido-2′,3′-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus
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Based on the promising drug resistance profile and potent anti-HIV activity of β-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.
- Zhang, Hong-wang,Coats, Steven J.,Bondada, Lavanya,Amblard, Franck,Detorio, Mervi,Asif, Ghazia,Fromentin, Emilie,Solomon, Sarah,Obikhod, Aleksandr,Whitaker, Tony,Sluis-Cremer, Nicolas,Mellors, John W.,Schinazi, Raymond F.
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scheme or table
p. 60 - 64
(2010/04/05)
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- 3'-AZIDO PURINE NUCLEOTIDE PRODRUGS FOR TREATMENT OF VIRAL INFECTIONS
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The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HIV, and HBV, in human patients or other animal hosts. The compounds are 3'-azido-2',3'-dideoxy purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1 and HBV.
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Page/Page column 53
(2010/07/02)
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- Nucleic acid related compounds. 57. Synthesis, X-ray crystal structure, lipophilic partition properties, and antiretroviral activities of anomeric 3'-azido-2',3'-dideoxy-2,6-diaminopurine ribosides
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Trimethylsilyl triflate-catalyzed transfer glycosylation of 2,6-diacetamidopurine (2) with 3'-azido-3'-deoxythymidine (AZT, 1) as donor followed by deprotection gave 2,6-diamino-9-(3-azido-2,3-dideoxy-α- and -β-D-erythro-pentofuranosyl)purines (3 and 4) i
- Robins,Wood,Dalley,Herdewijn,Balzarini,De Clercq
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p. 1763 - 1768
(2007/10/02)
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