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  • Title: Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.
    Author: Micale N, Ettari R, Schirmeister T, Evers A, Gelhaus C, Leippe M, Zappalà M, Grasso S.
    Journal: Bioorg Med Chem; 2009 Sep 15; 17(18):6505-11. PubMed ID: 19709887.
    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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