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

doi:10.1016/j.bmcl.2012.07.069

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 journal › Article › peer-review

10 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 language	English (US)
Pages (from-to)	5915-5918
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	22
Issue number	18
DOIs	https://doi.org/10.1016/j.bmcl.2012.07.069
State	Published - Sep 15 2012
Externally published	Yes

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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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title = "Antiplasmodial activities of 4-aminoquinoline-statine compounds",

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.",

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note = "Funding Information: This work was supported by MIUR (PRIN2008 20084MMXN: Leads ad Attivit{\`a} 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. ",

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AU - Vaiana, Nadia

AU - Marzahn, Melissa

AU - Parapini, Silvia

AU - Liu, Peng

AU - Dell'Agli, Mario

AU - Pancotti, Andrea

AU - Sangiovanni, Enrico

AU - Basilico, Nicoletta

AU - Bosisio, Enrica

AU - Dunn, Ben M.

AU - Taramelli, Donatella

AU - Romeo, Sergio

N1 - 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.

PY - 2012/9/15

Y1 - 2012/9/15

N2 - 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.

AB - 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.

KW - Aminoquinolines

KW - Antimalarials

KW - Double drugs

KW - Plasmepsin inhibitors

KW - Plasmodium falciparum

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Antiplasmodial activities of 4-aminoquinoline-statine compounds

Abstract

Bibliographical note

Keywords

UN SDGs

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