Use of proline bioisosteres in potential HIV protease inhibitors: phenylalanine-2-thiophenoxy-3-pyrrolidinone: synthesis and anti-HIV evaluation.
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.
Kraus
J L
JL
Laboratoire de Chimie Biomoleculaire, Faculté des Sciences de Luminy, Université de la Méditerranée, Marseille, France. kraus@luminy.univ-mrs.fr
Bouygues
M
M
Courcambeck
J
J
Chermann
J C
JC
D015374:Biosensing Techniques; D002460:Cell Line; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011392:Proline; D011760:Pyrrolidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D017320:HIV Protease Inhibitors; D011760:Pyrrolidinones; D011392:Proline