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.File in questo prodotto:
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