Antiplasmodial activities of 4-aminoquinoline-statine compounds

Nadia Vaiana, Melissa Marzahn, Silvia Parapini, Peng Liu, Mario Dell'Agli, Andrea Pancotti, Enrico Sangiovanni, Nicoletta Basilico, Enrica Bosisio, Ben M. Dunn, Donatella Taramelli, Sergio Romeo

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)5915-5918
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number18
DOIs
StatePublished - Sep 15 2012
Externally publishedYes

Bibliographical note

Funding Information:
This work was supported by MIUR (PRIN2008 20084MMXN: Leads ad Attività Antimalarica di Origine Naturale: Isolamento, Ottimizzazione e Valutazione Biologica), and by the AntiMal project, funded under the sixth Framework Programme of the European Community (Contract No. IP-018834). The authors are solely responsible for its content, which does not represent the opinion of the European Community and the Community is not responsible for any use that might be made of the information contained herein.

Keywords

  • Aminoquinolines
  • Antimalarials
  • Double drugs
  • Plasmepsin inhibitors
  • Plasmodium falciparum

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