Lysine sulfonamides as novel HIV-protease inhibitors: Nε-Acyl aromatic α-amino acids

A series of lysine sulfonamide analogues bearing Nε-acyl aromatic amino acids were synthesized using an efficient synthetic route. Evaluation of these novel protease inhibitors revealed compounds with high potency against wild-type and multiple-protease inhibitor-resistant HIV viruses.

Graphical abstractA series of Nα-isobutyl-Nα-arylsulfonamido-(Nε-acyl aromatic amino acid)lysinol derivatives were prepared and evaluated as inhibitors of HIV protease and viral replication.Figure optionsDownload full-size imageDownload as PowerPoint slide