Evaluation of substituted phenalenone analogues as antiplasmodial agents

David Gutiérrez; Esther Ninoska Flores Quisbert Flores Quisbert; Teresa Abad-Grillo; Grant McNaughton-Smith

doi:10.1016/j.exppara.2013.08.008

Evaluation of substituted phenalenone analogues as antiplasmodial agents

David Gutiérrez, Esther Ninoska Flores Quisbert Flores Quisbert, Teresa Abad-Grillo, Grant McNaughton-Smith

Resultado de la investigación: Contribución a una revista › Artículo › revisión exhaustiva

23 Citas (Scopus)

Resumen

A set of derivatives encompassing structural modifications on the privileged phenalenone scaffold were assessed for their antiplasmodial activities against a strain of chloroquine sensitive Plasmodium falciparum F32. Two compounds exhibited considerable effects against the malaria parasite (IC₅₀≤1μg/mL), one of which maintained the same level of activity in a chloroquine-resistant strain. This is the first record of antiplasmodial activity on this type of scaffold, providing a new structural motif as a new lead for antimalarial activity.

Idioma original	Inglés
Páginas (desde-hasta)	456-458
Número de páginas	3
Publicación	Experimental Parasitology
Volumen	135
N.º	2
DOI	https://doi.org/10.1016/j.exppara.2013.08.008
Estado	Publicada - oct. 2013

Nota bibliográfica

Funding Information:
This work was supported by MINECO ( SAF 2012-37344-C03-01 ). N. Flores and D. Gutierrez are grateful to MAEC-AECID and project X.5 “Búsqueda, Obtención y Evaluación de Nuevos Agentes Antiparasitarios” CYTED (Iberoamerican Program of Science and Technology for Development), Subprogram.

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title = "Evaluation of substituted phenalenone analogues as antiplasmodial agents",

abstract = "A set of derivatives encompassing structural modifications on the privileged phenalenone scaffold were assessed for their antiplasmodial activities against a strain of chloroquine sensitive Plasmodium falciparum F32. Two compounds exhibited considerable effects against the malaria parasite (IC50≤1μg/mL), one of which maintained the same level of activity in a chloroquine-resistant strain. This is the first record of antiplasmodial activity on this type of scaffold, providing a new structural motif as a new lead for antimalarial activity.",

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note = "Funding Information: This work was supported by MINECO ( SAF 2012-37344-C03-01 ). N. Flores and D. Gutierrez are grateful to MAEC-AECID and project X.5 “B{\'u}squeda, Obtenci{\'o}n y Evaluaci{\'o}n de Nuevos Agentes Antiparasitarios” CYTED (Iberoamerican Program of Science and Technology for Development), Subprogram.",

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AU - Gutiérrez, David

AU - Flores Quisbert, Esther Ninoska Flores Quisbert

AU - Abad-Grillo, Teresa

AU - McNaughton-Smith, Grant

N1 - Funding Information: This work was supported by MINECO ( SAF 2012-37344-C03-01 ). N. Flores and D. Gutierrez are grateful to MAEC-AECID and project X.5 “Búsqueda, Obtención y Evaluación de Nuevos Agentes Antiparasitarios” CYTED (Iberoamerican Program of Science and Technology for Development), Subprogram.

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N2 - A set of derivatives encompassing structural modifications on the privileged phenalenone scaffold were assessed for their antiplasmodial activities against a strain of chloroquine sensitive Plasmodium falciparum F32. Two compounds exhibited considerable effects against the malaria parasite (IC50≤1μg/mL), one of which maintained the same level of activity in a chloroquine-resistant strain. This is the first record of antiplasmodial activity on this type of scaffold, providing a new structural motif as a new lead for antimalarial activity.

AB - A set of derivatives encompassing structural modifications on the privileged phenalenone scaffold were assessed for their antiplasmodial activities against a strain of chloroquine sensitive Plasmodium falciparum F32. Two compounds exhibited considerable effects against the malaria parasite (IC50≤1μg/mL), one of which maintained the same level of activity in a chloroquine-resistant strain. This is the first record of antiplasmodial activity on this type of scaffold, providing a new structural motif as a new lead for antimalarial activity.

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KW - P. falciparum

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JO - Experimental Parasitology

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SN - 0014-4894

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Evaluation of substituted phenalenone analogues as antiplasmodial agents

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