Abstract
The synthesis of several new anti-HIV-1 compounds is described. The new compounds contain a C 2 symmetry axis and a dihidroxyethylene moiety based on the d-tartaric acid back bone. The synthesis of these compounds was achieved in 36–69% overall yields from d-tartaric acid. The protocol included: acetylation of hydroxyl groups, followed by diamide formation and deacetylation or reduction with LiAlH 4. The anti-HIV 1 activities of these substances were evaluated in PM-1 cells, using Indinavir® as standard (IC 50=0.2 μM). Two amino alcohol derivatives showed good inhibitory activity against the virus, with IC 50=2.0 and 4 μM.
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