Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors

…, T Schirmeister, A Evers, C Gelhaus, M Leippe…

文献索引：Micale, Nicola; Ettari, Roberta; Schirmeister, Tanja; Evers, Astrid; Gelhaus, Christoph; Leippe, Matthias; Zappala, Maria; Grasso, Silvana Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 18 p. 6505 - 6511

全文：HTML全文

被引用次数: 22

摘要

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 ...