2. Academic Validation
  3. Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline

Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline

  • Bioorg Med Chem Lett. 2008 Jul 1;18(13):3737-40. doi: 10.1016/j.bmcl.2008.05.042.
Anna Sparatore 1,  Nicoletta Basilico,  Manolo Casagrande,  Silvia Parapini,  Donatella Taramelli,  Reto Brun,  Sergio Wittlin,  Fabio Sparatore
Affiliations

Affiliation

  • 1 Istituto di Chimica Farmaceutica e Tossicologica Pietro Pratesi, University of Milan, Via Mangiagalli 25, 20133 Milan, Italy. anna.sparatore@unimi.it
PMID: 18538567 DOI: 10.1016/j.bmcl.2008.05.042
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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