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HIV-1 protease inhibitors containing a novel C2 symmetrical hydroxyalkylgem-diamino core structure
M Marastoni1, S Salvadori, F Bortolotti
1Department of Pharmaceutical Sciences, University of Ferrara, Italy.
Abstract:
Two series of peptidomimetics containing a novel C2 symmetrical hydroxyalkylgem-diamino core structure were prepared, from amino acid starting materials, and evaluated as inhibitors of HIV-1 protease (HIV-1 Pr). 1,1-Diamino-3-hydroxypropane (gHse) derivatives showed weak inhibitory potency (IC50 > 10 microM). In the 1,1-diamino-2-hydroxyethane (gSer) series, a compound containing P1/P1' benzyl and P2/P2'Fmoc substituents, displayed a significant HIV-1 Pr inhibition (IC50 = 440 nM).