| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375240 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
Abstract
Two pyrrolizidinylalkyl derivatives of 4-amino-7-chloroquinoline (MG2 and MG3) were prepared and tested in vitro against CQ-sensitive and CQ-resistant strains of Plasmodium falciparum and in vivo in a Plasmodium berghei mouse model of infection. Both compounds exhibited excellent activity in all tests and low toxicity against mammalian cells. Preliminary studies of the acute toxicity and of the metabolism of the most active compound MG3 indicate a promising profile as a new antimalarial drug candidate.
Graphical abstractNew orally efficacious chloroquine analogs with excellent activity on CQ-R strains of P. falciparum.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Anna Sparatore, Nicoletta Basilico, Manolo Casagrande, Silvia Parapini, Donatella Taramelli, Reto Brun, Sergio Wittlin, Fabio Sparatore,