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Ronchi, R.J.; Beaufay, C.; Bero, J.; Robirosa, J.B.; Mazzuca, M.; Palermo, J.A.; Quetin-Leclercq, J.; Sánchez, M. "Secochiliolide ester derivatives: Preparation and evaluation of their antitrypanosomal and antimalarial efficacy" (2018) Chemical Biology and Drug Design
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Abstract:

In the present study, a series of new esters of secochiliolide acid (SA), a diterpene isolated from Nardophyllum bryoides, were synthesized in good yield. All compounds were evaluated for their in vitro antiparasitic properties (on Plasmodium falciparum and Trypanosoma brucei brucei) and cytotoxicity (on WI38, normal mammalian cells). They displayed moderate antitrypanosomal activity with IC50 values between 2.55 and 18.14 μm, with selectivity indices >10, and low antiplasmodial effects with IC50 > 29 μm. The only exception was the n-hexyl ester of SA, which showed a strong and selective antiplasmodial activity (IC50 = 1.99 μm and selectivity index = 117.0). The in vivo antimalarial efficacy of this compound was then assessed according to the 4-day suppressive test of Peters in mice. An intraperitoneal treatment at 50 mg kg−1 day−1 induced a slight parasitaemia reduction by 56% which was statistically significant on day 4 post-infection and an increase in the survival time. © 2018 John Wiley & Sons A/S

Registro:

Documento: Artículo
Título:Secochiliolide ester derivatives: Preparation and evaluation of their antitrypanosomal and antimalarial efficacy
Autor:Ronchi, R.J.; Beaufay, C.; Bero, J.; Robirosa, J.B.; Mazzuca, M.; Palermo, J.A.; Quetin-Leclercq, J.; Sánchez, M.
Filiación:Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Buenos Aires, Argentina
Unidad de Microanálisis y Métodos Físicos en Química Orgánica (UMYMFOR), CONICET-Universidad de Buenos Aires, Buenos Aires, Argentina
Pharmacognosy Research Group, Louvain Drug Research Institute, Université catholique de Louvain, Brussels, Belgium
Departamento de Química, Facultad de Ciencias Naturales, Consejo Nacional de Investigaciones Científicas y Técnicas, Centro de Investigación y Transferencia Golfo San Jorge (CIT-Golfo San Jorge), Comodoro Rivadavia, Chubut, Argentina
Palabras clave:antimalarial efficacy; antiplasmodial activity; cytotoxicity; diterpene; Nardophyllum bryoides; secochiliolide acid esters
Año:2018
DOI: http://dx.doi.org/10.1111/cbdd.13392
Título revista:Chemical Biology and Drug Design
Título revista abreviado:Chem. Biol. Drug Des.
ISSN:17470277
CODEN:CBDDA
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_17470277_v_n_p_Ronchi

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Citas:

---------- APA ----------
Ronchi, R.J., Beaufay, C., Bero, J., Robirosa, J.B., Mazzuca, M., Palermo, J.A., Quetin-Leclercq, J.,..., Sánchez, M. (2018) . Secochiliolide ester derivatives: Preparation and evaluation of their antitrypanosomal and antimalarial efficacy. Chemical Biology and Drug Design.
http://dx.doi.org/10.1111/cbdd.13392
---------- CHICAGO ----------
Ronchi, R.J., Beaufay, C., Bero, J., Robirosa, J.B., Mazzuca, M., Palermo, J.A., et al. "Secochiliolide ester derivatives: Preparation and evaluation of their antitrypanosomal and antimalarial efficacy" . Chemical Biology and Drug Design (2018).
http://dx.doi.org/10.1111/cbdd.13392
---------- MLA ----------
Ronchi, R.J., Beaufay, C., Bero, J., Robirosa, J.B., Mazzuca, M., Palermo, J.A., et al. "Secochiliolide ester derivatives: Preparation and evaluation of their antitrypanosomal and antimalarial efficacy" . Chemical Biology and Drug Design, 2018.
http://dx.doi.org/10.1111/cbdd.13392
---------- VANCOUVER ----------
Ronchi, R.J., Beaufay, C., Bero, J., Robirosa, J.B., Mazzuca, M., Palermo, J.A., et al. Secochiliolide ester derivatives: Preparation and evaluation of their antitrypanosomal and antimalarial efficacy. Chem. Biol. Drug Des. 2018.
http://dx.doi.org/10.1111/cbdd.13392