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  • Title: Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors.
    Author: Bova F, Ettari R, Micale N, Carnovale C, Schirmeister T, Gelhaus C, Leippe M, Grasso S, Zappalà M.
    Journal: Bioorg Med Chem; 2010 Jul 15; 18(14):4928-38. PubMed ID: 20598553.
    Abstract:
    Herein we report the synthesis of a series of novel constrained peptidomimetics 2-10 endowed with a dipeptide backbone (D-Ser-Gly) and a vinyl ester warhead, structurally related to a previously identified lead compound 1, an irreversible inhibitor of falcipain-2, the main haemoglobinase of lethal malaria parasite Plasmodium falciparum. The new compounds were evaluated for their inhibition against falcipain-2, as well as against cultured P. falciparum. The inhibitory activity of the synthesized compounds was also evaluated against another protozoal cysteine protease, namely rhodesain of Trypanosoma brucei rhodesiense.
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