Secochiliolide ester derivatives: Preparation and evaluation of their antitrypanosomal and antimalarial efficacy.
(2019) Chemical Biology & Drug Design (Print) — Vol. 93, n° 2, p. 147-153 (2019)
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- Authors
Sánchez, Marianela 
- 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 IC values between 2.55 and 18.14 μm, with selectivity indices >10, and low antiplasmodial effects with IC > 29 μm. The only exception was the n-hexyl ester of SA, which showed a strong and selective antiplasmodial activity (IC = 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 day induced a slight parasitaemia reduction by 56% which was statistically significant on day 4 post-infection and an increase in the survival time.
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Citations
Ronchi, R. J., Beaufay, C., Bero, J., Robirosa, J. B., Mazzuca, M., Palermo, J. A., Quetin-Leclercq, J., & Sánchez, M. (2019). Secochiliolide ester derivatives: Preparation and evaluation of their antitrypanosomal and antimalarial efficacy. Chemical Biology & Drug Design (Print), 93(2), 147-153. https://doi.org/10.1111/cbdd.13392 (Original work published 2019)