Synthesis of N-glyoxylyl peptides and their in vitro evaluation as HIV-1 protease inhibitors

…, I Vergely, N Boggetto, M Reboud-Ravaux

Index: Qasmi, Driss; De Rosny, Eve; Rene, Loic; Badet, Bernard; Vergely, Isabelle; Boggetto, Nicole; Reboud-Ravaux, Michele Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 4 p. 707 - 714

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Citation Number: 13

Abstract

A series of novel synthetic peptides containing an N-terminal glyoxylyl function (CHOCO-) have been tested as inhibitors of HIV-1 protease. The N-glyoxylyl peptide CHOCO-Pro-He- Val-NH2, which fulfills the specificity requirements of the MA/CA protease cleavage site together with the criteria of transition state analogue of the catalyzed reaction, was found to be a moderate competitive inhibitor although favorable interactions were visualized ...