204381-62-4Relevant articles and documents
Parallel synthesis of new phenylalanino-2-(phenylthio)pyrrolidin-3-one scaffold-based analogues
Quelever, Gilles,Bouygues, Martin,Kraus, Jean-Louis
, p. 1181 - 1189 (2007/10/03)
Based on the specific PhePro proteolytic cleavage of the HIV-protease, we synthesized short pseudopeptides incorporating a 2-(phenylthio)pyrrolidin-3-one ring. We previously described various analogues based on this scaffold. We report herein a parallel m
Short and unexpectedly potent 3-pyrrolidinone type inhibitors of HIV-1 replication
Bouygues, Martin,Medou, Martial,Chermann, Jean-Claude,Camplo, Michel,Kraus, Jean-Louis
, p. 445 - 450 (2007/10/03)
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.