Synthesis, In Vitro Anti-HIV and Anti-hepatitis B Activities and Pharmacokinetic Properties of Amphiphilic Heterodinucleoside Phosphates Containing ddC and AZT

Amphiphilic heterodinucleoside phosphates containing AZT and ddC as antiviral monomer were synthesized according to the hydrogenphosphonate method and evaluated in vitro against HIV. dT-N 4 -pamddC was the most active (IC 50 = 40 μM, EC 50 = 80 nM) and least toxic (TI = 524) dimer and it exhibited a...

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Published inNucleosides & nucleotides Vol. 18; no. 4-5; pp. 949 - 950
Main Authors Schwendener, R. A., Peghini, P. A., Ludwig, P. S., Schott, H.
Format Journal Article
LanguageEnglish
Published United States Taylor & Francis Group 01.04.1999
Subjects
Anti-HIV Agents - chemical synthesis
Anti-HIV Agents - pharmacology
Antiviral Agents - chemical synthesis
Antiviral Agents - pharmacology
Cell Line
Hepatitis B virus - drug effects
Hepatitis B virus - physiology
HIV-1 - drug effects
Humans
Microbial Sensitivity Tests
Virus Replication - drug effects
Zalcitabine - analogs & derivatives
Zalcitabine - chemical synthesis
Zalcitabine - pharmacology
Zidovudine - analogs & derivatives
Zidovudine - chemical synthesis
Zidovudine - pharmacology
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Summary:Amphiphilic heterodinucleoside phosphates containing AZT and ddC as antiviral monomer were synthesized according to the hydrogenphosphonate method and evaluated in vitro against HIV. dT-N 4 -pamddC was the most active (IC 50 = 40 μM, EC 50 = 80 nM) and least toxic (TI = 524) dimer and it exhibited also strong antiviral effects against eight AZT-resistant HIV strains. The ddC-containing heterodimers additionally inhibited HBV replication by 50-80% at 50 μM in Hep G2 2.2.15 cells.
ISSN:0732-8311
2332-3892
DOI:10.1080/15257779908041609