Synthesis and anti-HIV activity of alpha-thiophenoxy-hydroxyethylamide derivatives

A series of new anti-MN derivatives containing a novel alpha-thiophenoxyhyd roxyethylamide core have been synthesized, using S-phenylbenzenethiosulfona te as the thiosulfenylating reagent. Some of the new synthesized compounds (1a, 1c, 1g, 1i, 1j and 1l) inhibited HIV replication in cell culture assay s (syncytia formation) with effective concentrations (EC50) ranging from 0. 1-1 mu M Incorporation of thiophenoxy substitution within various pseudomim etic peptide backbones provided a series of highly potent HN inhibitors. (C ) 1999 Editions sicentifiques et medicales Elsevier SAS.