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  • Title: HIV protease inhibitors: synthesis and activity of N-aryl-N'-hydroxyalkyl hydrazide pseudopeptides.
    Author: Marastoni M, Baldisserotto A, Trapella C, McDonald J, Bortolotti F, Tomatis R.
    Journal: Eur J Med Chem; 2005 May; 40(5):445-51. PubMed ID: 15893018.
    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 microM) and exhibited enzymatic resistance and stability in vitro.
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