TY - JOUR
T1 - HIV-1 protease inhibitors containing an N-Hydroxyamino acid core structure
AU - Marastoni, Mauro
AU - Bazzaro, Martina
AU - Salvadori, Severo
AU - Bortolotti, Fabrizio
AU - Tomatis, Roberto
N1 - 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.
PY - 2001/4
Y1 - 2001/4
N2 - 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.
AB - 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.
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U2 - 10.1016/S0968-0896(00)00308-4
DO - 10.1016/S0968-0896(00)00308-4
M3 - Article
C2 - 11354677
AN - SCOPUS:0035034179
SN - 0968-0896
VL - 9
SP - 939
EP - 945
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 4
ER -
