Abstract
| - A series of new polyanions was synthesized viaγ-polymerization, in aqueous micellar solution,of ω-unsaturated anionic surfactants whose polar head was derivedfrom amino acids ordipeptides. The obtained polyanions were evaluated for theiractivity against humanimmunodeficiency virus (HIV-1, HIV-2) and various other RNA and DNAviruses. All the testcompounds proved active against HIV-1 and HIV-2, their 50% inhibitoryconcentration (IC50)being in the range of 0.04−7.5 μg/mL, while they were not toxic tothe host cells (CEM-4 orMT-4) at concentrations up to 100 μg/mL or higher. TheHIV-inhibitory effect increased withthe hydrophilic character of the amino acid moiety. The compoundswere found to interactwith both the viral envelope glycoprotein gp120 and the cellular CD4receptor, thus blockingvirus−cell binding and virus-induced syncytium formation. Thesepolyanions also proved activeagainst human cytomegalovirus at about the same IC50 as forHIV. In addition, they werealso active, albeit at somewhat higher IC50 values(0.8−20 μg/mL), against other envelopedviruses such as respiratory syncytial virus and arenaviruses (Junin andTacaribe). At yethigher IC50 values (≥20 μg/mL), some of the compoundsshowed activity against influenza Avirus. No activity was observed with any of the compounds againstvesicular stomatitis virus,Sindbis virus, Semliki forest virus, influenza B, parainfluenza type 3,and the nonenvelopedviruses Coxsackie type B4, polio type 1, and reovirus type1.
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