Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline

作者：Sparatore Anna^*; Basilico Nicoletta; Casagrande Manolo; Parapini Silvia; Taramelli Donatella; Brun Reto; Wittlin Sergio; Sparatore Fabio

来源：Bioorganic & Medicinal Chemistry Letters, 2008, 18(13): 3737-3740.

DOI：10.1016/j.bmcl.2008.05.042

• 4-aminoquinoline derivatives
• pyrrolizidinyl derivatives
• chloroquine
• antimalarial agents

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 pro. le as a new antimalarial drug candidate.

• 出版日期2008-7-1