54837-25-1Relevant articles and documents
HIV-1 protease inhibitors containing an N-Hydroxyamino acid core structure
Marastoni, Mauro,Bazzaro, Martina,Salvadori, Severo,Bortolotti, Fabrizio,Tomatis, Roberto
, p. 939 - 945 (2001)
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. Copyright
