Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors |
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| Authors: | Nicola Micale Roberta Ettari Tanja Schirmeister Astrid Evers Christoph Gelhaus Matthias Leippe Maria Zappal Silvana Grasso |
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| Institution: | aDipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata 98168, Messina, Italy;bInstitute of Pharmacy and Food Chemistry, University of Würzburg Am Hubland, 97074 Würzburg, Germany;cZoological Institute, University of Kiel, Olshausenstrasse 40, D-24098 Kiel, Germany |
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| Abstract: | A series of 1-aryl-6,7-disubstituted-2H-isoquinolin-3-ones (2–10) was synthesized and evaluated for their inhibition against Plasmodium falciparum cysteine protease falcipain-2, as well as against cultured P. falciparum strain FCBR parasites. All compounds displayed inhibitory activity against recombinant falcipain-2 and against in vitro cultured intraerythrocytic P. falciparum, with the exception of 9. The new compounds exhibited no selectivity against human cysteine proteases such as cathepsins B and L. 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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| Keywords: | Cysteine proteases Falcipain-2 inhibitors 2H-Isoquinolin-3-ones |
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