We report the discovery of new potent inhibitors of the growth of Plasmodium falciparum chloroquine (CQ)-resistant W2 strain. These compounds were designed using the double drug approach by introducing a residue able to enhance the accumulation of plasmepsins inhibitors into the food vacuole. Some of the molecules were more active than CQ against CQ-resistant strain and showed good selectivity against cathepsin D.

Antiplasmodial activities of 4-aminoquinoline–statine compounds / N. Vaiana, M. Marzahn, S. Parapini, P. Liu, M. Dell’Agli, A. Pancotti, E. Sangiovanni, N. Basilico, E. Bosisio, B.M. Dunn, D. Taramelli, S. Romeo. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 22:18(2012), pp. 5915-5918.

Antiplasmodial activities of 4-aminoquinoline–statine compounds

N. Vaiana
Primo
;
S. Parapini;M. Dell’Agli;A. Pancotti;E. Sangiovanni;N. Basilico;E. Bosisio;D. Taramelli
Penultimo
;
S. Romeo
Ultimo
2012

Abstract

We report the discovery of new potent inhibitors of the growth of Plasmodium falciparum chloroquine (CQ)-resistant W2 strain. These compounds were designed using the double drug approach by introducing a residue able to enhance the accumulation of plasmepsins inhibitors into the food vacuole. Some of the molecules were more active than CQ against CQ-resistant strain and showed good selectivity against cathepsin D.
Aminoquinolines; Antimalarials; Double drugs; Plasmepsin inhibitors; Plasmodium falciparum
Settore CHIM/08 - Chimica Farmaceutica
Settore BIO/15 - Biologia Farmaceutica
Settore MED/04 - Patologia Generale
Settore MED/07 - Microbiologia e Microbiologia Clinica
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/203786
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