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Nucleic Acids, Nucleotides, and Nucleosides Commons™
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- 4-acetoxybenzyl alcohols (1)
- 5¢-O-b (1)
- Anti-HIV activity (1)
- Ester conjugates of TFV (1)
- Fatty chains (1)
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- G-methylenetriphosphates (1)
- HIV-1 inhibitory activity (1)
- HIV-1 reverse transcriptase (1)
- Isosteric P–CH2–P bond (1)
- Nucleosides (1)
- Nucleotides (1)
- Phosphate transfer (1)
- Phosphonamidate (1)
- Polystyrene resinbound linkers (1)
- Pronucleotides (1)
- RNase H activity (1)
- Tenofovir (TFV) (1)
- Tenofovir alafenamide (TAF) (1)
- Triphosphotriesters (1)
Articles 1 - 3 of 3
Full-Text Articles in Nucleic Acids, Nucleotides, and Nucleosides
Synthesis And Evaluation Of Anti-Hiv Activity Of Mono- And Di-Substituted Phosphonamidate Conjugates Of Tenofovir, Aaminat Qureshi, Louise A. Ouattara, Naglaa Salem El-Sayed, Amita Verma, Gustavo F. Doncel, Muhammad Iqbal Choudhary, Hina Siddiqui, Keykavous Parang
Synthesis And Evaluation Of Anti-Hiv Activity Of Mono- And Di-Substituted Phosphonamidate Conjugates Of Tenofovir, Aaminat Qureshi, Louise A. Ouattara, Naglaa Salem El-Sayed, Amita Verma, Gustavo F. Doncel, Muhammad Iqbal Choudhary, Hina Siddiqui, Keykavous Parang
Pharmacy Faculty Articles and Research
The activity of nucleoside and nucleotide analogs as antiviral agents requires phosphorylation by endogenous enzymes. Phosphate-substituted analogs have low bioavailability due to the presence of ionizable negatively-charged groups. To circumvent these limitations, several prodrug approaches have been proposed. Herein, we hypothesized that the conjugation or combination of the lipophilic amide bond with nucleotide-based tenofovir (TFV) (1) could improve the anti-HIV activity. During the current study, the hydroxyl group of phosphonates in TFV was conjugated with the amino group of L-alanine, L-leucine, L-valine, and glycine amino acids and other long fatty ester hydrocarbon chains to synthesize 43 derivatives. Several …
Synthesis Of Β-Triphosphotriester Pronucleotides, Yousef A. Beni, Chandravanu Dash, Keykavous Parang
Synthesis Of Β-Triphosphotriester Pronucleotides, Yousef A. Beni, Chandravanu Dash, Keykavous Parang
Pharmacy Faculty Articles and Research
Dinucleoside phosphorochloridite were synthesized from phosphorus trichloride and three nucleoside analogues, 3-fluoro-2,3-dideoxythymidine (FLT), 2',3'-dideoxy-5-fluoro-3'- thiacytidine (FTC), and 2',3'-dideoxy-3'-thiacytidine (3TC), in a multistep synthesis. Polymerbound N-Boc p-acetoxybenzyl 5¢-O-2¢-deoxythymidine was reacted with dinucleoside phosphorochloridite in the presence of 2,6-lutidine, followed by the reaction with dodecyl alcohol and 5-(ethylthio)-1H-tetrazole, oxidation with tert-butyl hydroperoxide, and acidic cleavage, respectively, to afford the b-triphosphotriester derivatives containing three different nucleosides.
5¢-O-B,G-Methylenetriphosphate Derivatives Of Nucleoside, Yousef Ahmadibeni, Chandravanu Dash, S. F. J. Le Grice, Keykavous Parang
5¢-O-B,G-Methylenetriphosphate Derivatives Of Nucleoside, Yousef Ahmadibeni, Chandravanu Dash, S. F. J. Le Grice, Keykavous Parang
Pharmacy Faculty Articles and Research
The solid-phase synthesis of 5¢-O-b,g-methylenetriphosphates of nucleosides 1–5 is described, where a 4-acetoxy-3-arylbenzyloxy group was used as a linker.