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'-hydrogenphosphonate. The corresponding derivatives of d2A and d4T showed the same properties.
Khandazhinskaya
A L
AL
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, Russian Federation.
Shirokova
E A
EA
Karpenko
I L
IL
Zakirova
N F
NF
Tarussova
N B
NB
Krayevsky
A A
AA
D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000737:chemistry*; D003692:Delayed-Action Preparations; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D063065:Organophosphonates / Q000737:chemistry*; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000737:chemistry*; D015215:Zidovudine / Q000008:administration & dosage* / Q000737:chemistry*
D019380:Anti-HIV Agents; D003692:Delayed-Action Preparations; D063065:Organophosphonates; D018894:Reverse Transcriptase Inhibitors; D015215:Zidovudine