SHORT AND UNEXPECTEDLY POTENT 3-PYRROLIDINONE TYPE INHIBITORS OF HIV-1 REPLICATION

Based on the specific PhePro proteolytic cleavage of the HIV protease, short pseudo-peptides incorporating a 3-pyrrolidinone 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 BocP hePro. Analogues incorporating an aromatic residue have shown to inhib it HIV-1 infection in MT4 human lymphoid cell with an IC50 ranging fro m 1 to 10 mu M. Further experiments are in progress to determine their HIV protease inhibition properties. (C) Elsevier, Paris.