HIV-1 protease inhibitors containing an N-Hydroxyamino acid core structure

Mauro Marastoni, Martina Bazzaro, Severo Salvadori, Fabrizio Bortolotti, Roberto Tomatis

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17 Scopus citations


Two series of peptidomimetics containing an N-hydroxyamino acid core structure were prepared by mixed solution solid-phase synthesis and tested for inhibitory activity against the human immunodeficiency virus (HIV-1) protease (Pr) and the virus in cell culture. In general, N-hydroxy Gly containing pseudopeptides displayed modest HIV Pr inhibition (IC50≥930 nM). In the N-hydroxy Phe derivatives, Fmoc-Phe-ψ[(CO-N OH)]-Phe-Pro-NHtBu was the best inhibitor of the series IC50 = 144nM showing satisfactory inhibition of HIV replication in cell culture (ED50 = 98 nM) and remarkable stability against cell culture and plasma enzymes.

Original languageEnglish (US)
Pages (from-to)939-945
Number of pages7
JournalBioorganic and Medicinal Chemistry
Issue number4
StatePublished - Apr 2001

Bibliographical note

Funding Information:
Financial support of this work by University of Ferrara and by Ministero dell'Università e della Ricerca Scientifica e Tecnologica (MURST) is gratefully acknowledged.


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