Short and unexpectedly potent 3-pyrrolidinone type inhibitors of HIV-1 replication

Article abstract of DOI:10.1016/S0223-5234(98)80045-7

Based on the specific PhePro proteolytic cleavage of the HIV protease, short pseudo-peptides incorporating a 3-pyrrolidinone none ring have been synthesized. Their potencies to inhibit HIV-1 in MT₄ cell culture have been evaluated and compared to that of the bioisostere dipeptide BocPhePro. Analogues incorporating an aromatic residue have shown to inhibit HIV-1 infection in MT₄ human lymphoid cell with an IC₅₀ ranging from 1 to 10 μM. Further experiments are in progress to determine their HIV protease inhibition properties.