POLYANION INHIBITORS OF HUMAN-IMMUNODEFICIENCY-VIRUS AND OTHER VIRUSES .6. MICELLE-LIKE ANTI-HIV POLYANIONIC COMPOUNDS BASED ON A CARBOHYDRATE CORE

A new class of polyanionic compounds, inhibitors of human immunodefici ency virus, was obtained from radical addition of mercapto acid or mer capto ester on a perallylated carbohydrate under UV irradiation with a catalytic amount of AIBN. Unlike the polyanions that we have previous ly prepared by polymerization reactions, the compounds are structurall y well defined. Polyanions bearing 16 carboxylate groups showed a 50% inhibitory concentration (IC50) of 0.1-4.1 mu g/mL against HIV-1 in MT -4 cells while not being toxic to the host cells at concentrations up to 125 mu g/mL. The most potent polyanions also proved active against human cytomegalovirus at concentrations of 1-14 mu g/mL. No activity w as observed against any of the other viruses tested (i.e., herpes simp lex virus, vesicular stomatitis virus, Sindbis, Semliki forest, parain fluenza-3, Junin, Tacaribe, Coxsackie B4, polio-1, reo-1, or vaccinia virus).