The design, synthesis, and antiplasmodial activity of antimalarial heterodimers based on the 1,4-bis(3-aminopropyl)piperazine linker is reported. In this series key structural elements derived from quinoline antimalarials were coupled to fragments capable of coordinating metal ions. Biological evaluation included determination of activity against chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum strains. Some of the novel compounds presented high activity in vitro against chloroquine-resistant strains, more potent than chloroquine and clotrimazole. Computational studies revealed that the activity is likely due to the ability of the compounds to assume a multisite iron coordinating geometry

Development of piperazine-tethered heterodimers as potent antimalarials against chloroquine-resistant P. falciparum strains. Synthesis and molecular modeling / S., Gemma; G., Kukreja; G., Campiani; S., Butini; M., Bernetti; B. P., Joshi; L., Savini; N., Basilico; D., Taramelli; V., Ardley; Bertamino, Alessia; Novellino, Ettore; Persico, Marco; Catalanotti, Bruno; Fattorusso, Caterina. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 17:(2007), pp. 3535-3539. [10.1016/j.bmcl.2007.04.077]

Development of piperazine-tethered heterodimers as potent antimalarials against chloroquine-resistant P. falciparum strains. Synthesis and molecular modeling

BERTAMINO, ALESSIA;NOVELLINO, ETTORE;PERSICO, MARCO;CATALANOTTI, BRUNO;FATTORUSSO, CATERINA
2007

Abstract

The design, synthesis, and antiplasmodial activity of antimalarial heterodimers based on the 1,4-bis(3-aminopropyl)piperazine linker is reported. In this series key structural elements derived from quinoline antimalarials were coupled to fragments capable of coordinating metal ions. Biological evaluation included determination of activity against chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum strains. Some of the novel compounds presented high activity in vitro against chloroquine-resistant strains, more potent than chloroquine and clotrimazole. Computational studies revealed that the activity is likely due to the ability of the compounds to assume a multisite iron coordinating geometry
2007
Development of piperazine-tethered heterodimers as potent antimalarials against chloroquine-resistant P. falciparum strains. Synthesis and molecular modeling / S., Gemma; G., Kukreja; G., Campiani; S., Butini; M., Bernetti; B. P., Joshi; L., Savini; N., Basilico; D., Taramelli; V., Ardley; Bertamino, Alessia; Novellino, Ettore; Persico, Marco; Catalanotti, Bruno; Fattorusso, Caterina. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 17:(2007), pp. 3535-3539. [10.1016/j.bmcl.2007.04.077]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/108119
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