We describe the synthesis and activities of a series of pseudopeptides containing an N-aryl-N′-hydroxyalkyl hydrazide core structure to inhibit human immunodeficiency virus protease and viral replication. Of the series, compound Hmb-Leu-N(Bzl)-N(CH2-CH-OH)-rPro-Boc (24) displayed the greatest inhibitory potency (IC50 < 1 μM) and exhibited enzymatic resistance and stability in vitro.

HIV protease inhibitors: synthesis and activity of N-aryl-N '-hydroxyalkyl hydrazide pseudopeptides

MARASTONI, Mauro;BALDISSEROTTO, Anna;TRAPELLA, Claudio;BORTOLOTTI, Fabrizio;TOMATIS, Roberto
2005

Abstract

We describe the synthesis and activities of a series of pseudopeptides containing an N-aryl-N′-hydroxyalkyl hydrazide core structure to inhibit human immunodeficiency virus protease and viral replication. Of the series, compound Hmb-Leu-N(Bzl)-N(CH2-CH-OH)-rPro-Boc (24) displayed the greatest inhibitory potency (IC50 < 1 μM) and exhibited enzymatic resistance and stability in vitro.
Marastoni, Mauro; Baldisserotto, Anna; Trapella, Claudio; Mcdonald, J; Bortolotti, Fabrizio; Tomatis, Roberto
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/1196692
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