abstract |
The present invention relates to a class of compounds which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of mannitol-derived HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features represented by formula (I), each A and A' is independently selected from the group consisting of a naturally occurring alpha-amino acid and an unnatural alpha-amino acid (e.g., whereineach n is independently selected from the group consisting of 0, 1 and 2; wherein each B and B' is independently selected from the group consisting of oxygen and sulfur; wherein each D and D' is independently selected from the group consisting of H2, oxygen and sulfur; wherein each E and E' is independently selected from the group consisting of Ar and N (R11R12). The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting the activity of HIV aspartyl protease. Accordingly, they may be advantageously used as anti-viral agents against HIV viruses, including the HIV-1 and HIV-2 viruses. |