Synthesis and antiherpetic activity of acyclovir phosphonates.
Phosphonate derivatives of acyclovir containing phosphorous acid and ethoxycarbonylphosphonic acid residues as well as their isopropyl esters were prepared. They selectively inhibited the herpes simplex virus 1 reproduction in Vero cell culture, the efficacy of esters being 3-4 times higher than that of ACV. The hydrolysis of the synthesized compounds was studied in the PBS buffer and human blood serum.
Karpenko
Inna L
IL
Engelhardt Institute of Molecular Biology, Russian Academy of Medical Sciences, Moscow, Russian Federation.
Jasko
Maxim V
MV
Andronova
Valeriya L
VL
Ivanov
Alexander V
AV
Kukhanova
Marina K
MK
Galegov
Georgy A
GA
Skoblov
Yury S
YS
D000212:Acyclovir / Q000097:blood / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D018259:Herpesvirus 1, Human / Q000187:drug effects* / Q000254:growth & development; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D010755:Organophosphates / Q000097:blood / Q000737:chemistry; D063065:Organophosphonates / Q000737:chemistry*; D014709:Vero Cells
D000998:Antiviral Agents; D010755:Organophosphates; D063065:Organophosphonates; D000212:Acyclovir