P-(Alkyl)-Nucleoside 5′-Hydrogenphosphonates as Depot Forms of Antiviral Nucleotide Analogues

P-(Alkyl)esters of AZT 5′-hydrogenphosphonate were synthesized and their stabilities in the phosphate buffer and human serum were evaluated. The esters bearing residues of primary and secondary alcohols were degraded to give AZT, whereas those containing tertiary alkyl groups yielded AZT 5′-hydrogen...

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Veröffentlicht in:	Nucleosides, nucleotides & nucleic acids nucleotides & nucleic acids, 2000-10, Vol.19 (10-12), p.1795-1804
Hauptverfasser:	Khandazhinskaya, A. L., Shirokova, E. A., Karpenko, I. L., Zakirova, N. F., Tarussova, N. B., Krayevsky, A. A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-HIV Agents - administration & dosage Anti-HIV Agents - chemistry Delayed-Action Preparations Humans Magnetic Resonance Spectroscopy Organophosphonates - chemistry Reverse Transcriptase Inhibitors - administration & dosage Reverse Transcriptase Inhibitors - chemistry Zidovudine - administration & dosage Zidovudine - chemistry
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Beschreibung
Zusammenfassung:	P-(Alkyl)esters of AZT 5′-hydrogenphosphonate were synthesized and their stabilities in the phosphate buffer and human serum were evaluated. The esters bearing residues of primary and secondary alcohols were degraded to give AZT, whereas those containing tertiary alkyl groups yielded AZT 5′-hydrogenphosphonate. The corresponding derivatives of d2A and d4T showed the same properties.
ISSN:	1525-7770 1532-2335
DOI:	10.1080/15257770008045461