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Updated: Jun 27, 2026
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Synthesis and antiplasmodial activity of 6H,13H-pyrazino[1,2-a;4,5-a']diindole analogues substituted with basic side
Darius P Zlotos1, Siegrid Franke2, Che J Ngwa3
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, The German University in Cairo New Cairo City 11835 Cairo Egypt darius.zlotos@guc.edu.eg.
Abstract:
The synthesis of pentacyclic 6H,13H-pyrazino[1,2-a;4,5-a']diindole analogues and their evaluation for antiplasmodial activity against 3D7 Plasmodium falciparum strains using [3H]hypoxanthine incorporation and SYBR® Green assays are reported. While the unsubstituted analogues are characterized by only weak antimalarial activity, introduction of one or two basic side-chains led to substantially increased antiplasmodial activity and reduced cytotoxicity against macrophage J774.1 cells. Screening data on chloroquine-sensitive 3D7 and chloroquine-resistant Dd2 strains using the Malstat assay showed that compounds 18, 21 and 23 are characterized by nanomolar activity against both strains, making them promising leads for the development of new antimalarial agents against chloroquine-resistant Plasmodium.
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