Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors |
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| Authors: | Floriana Bova Roberta Ettari Nicola Micale Caterina Carnovale Tanja Schirmeister Christoph Gelhaus Matthias Leippe Silvana Grasso Maria Zappalà |
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| Institution: | 1. Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy;2. Institute of Pharmacy and Food Chemistry, University of Würzburg Am Hubland, 97074 Würzburg, Germany;3. Zoological Institute, University of Kiel, Olshausenstrasse 40, D-24098 Kiel, Germany |
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| 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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