Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme

Adult T-cell leukemia and tropical spastic paraparesis/HTLV-I-associated myelopathy are only some of the more common end results of an infection with a human T-cell leukemia virus type 1 (HTLV-I). Expanding from our previous reports, we synthesized all different permutations of tetrapeptidic HTLV-I protease inhibitors using at least eight P3-cap and five P1′-cap moieties. The inhibitors exhibited over 97% inhibition against HIV-1 protease and a wide range of inhibitory activity against HTLV-I protease.

Structure–activity relationship studies were performed on 44 novel tetrapeptidic HTLV-I protease inhibitors possessing different hydrophobic P3-cap and P1′-cap moieties.Figure optionsDownload as PowerPoint slide