Phosphoramidate derivatives of acyclovir: synthesis and antiviral activity in HIV-1 and HSV-1 models in vitro.

Authors :: Zakirova NF
Shipitsyn AV
Jasko MV
Prokofjeva MM
Andronova VL
Galegov GA
Prassolov VS
Kochetkov SN
Source :: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2012 Oct 01; Vol. 20 (19), pp. 5802-9. Date of Electronic Publication: 2012 Aug 17.
Publication Year :: 2012
Abstract: The antiviral activity against HIV and HSV and the chemical stability of ACV phosphoramidate derivatives were studied. The phosphoramidates of ACV demonstrated moderate activity. The best compound appeared to be 9-(2-hydroxymethyl)guanine phosphoromonomorpholidate (7), which inhibited virus replication in pseudo-HIV-1 particles by 50% at 50 μM. It also inhibited replication of wild-type HSV-1 (9.7 μM) as well as an acyclovir-resistant strain (25 μM). None of the synthesised compounds showed any cytotoxicity.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Subjects :: Acyclovir chemical synthesis
Animals
Antiviral Agents chemical synthesis
Chlorocebus aethiops
HEK293 Cells
HIV Infections drug therapy
Herpes Simplex drug therapy
Humans
Vero Cells
Virus Replication drug effects
Acyclovir analogs & derivatives
Acyclovir pharmacology
Antiviral Agents chemistry
Antiviral Agents pharmacology
HIV-1 drug effects
Herpesvirus 1, Human drug effects

Full Text Access

Tools