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.
Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline / A. Sparatore, N. Basilico, M. Casagrande, S. Parapini, D. Taramelli, R. Brun, S. Wittlin, F. Sparatore. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 18:13(2008 Jul 01), pp. 3737-3740.
Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline
A. Sparatore
;N. BasilicoSecondo
;M. Casagrande;S. Parapini;D. Taramelli;
2008
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.
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