216392-37-9Relevant academic research and scientific papers
Use of proline bioisosteres in potential HIV protease inhibitors: Phenylalanine-2-thiophenoxy-3-pyrrolidinone: Synthesis and anti-HIV evaluation
Kraus,Bouygues,Courcambeck,Chermann
, p. 2023 - 2026 (2007/10/03)
The synthesis of new phenylalanine-2-thiophenoxy-3-pyrrolidinones is described. Anti-HIV recombinant protease assays and HIV infected cell culture assays (observation of syncytia) demonstrated the potent anti-HIV activity of this new class of pseudopeptides. (C) 2000 Published by Elsevier Science Ltd.
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.
