Antiplasmodial activities of 4-aminoquinoline–statine compounds

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 o...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2012-09, Vol.22 (18), p.5915-5918
Main Authors: Vaiana, Nadia, Marzahn, Melissa, Parapini, Silvia, Liu, Peng, Dell’Agli, Mario, Pancotti, Andrea, Sangiovanni, Enrico, Basilico, Nicoletta, Bosisio, Enrica, Dunn, Ben M., Taramelli, Donatella, Romeo, Sergio
Format: Article
Language:English
Subjects:
Amino Acids - chemistry
Amino Acids - pharmacology
Aminoquinolines
Aminoquinolines - chemistry
Aminoquinolines - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimalarials
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Antiparasitic agents
Biological and medical sciences
Cathepsin D - antagonists & inhibitors
Cathepsin D - metabolism
Dose-Response Relationship, Drug
Double drugs
Humans
Medical sciences
Molecular Structure
Parasitic Sensitivity Tests
Pharmacology. Drug treatments
Plasmepsin inhibitors
Plasmodium falciparum
Plasmodium falciparum - drug effects
Plasmodium falciparum - growth & development
Protease Inhibitors - chemical synthesis
Protease Inhibitors - chemistry
Protease Inhibitors - pharmacology
Structure-Activity Relationship
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.07.069