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Open AccessArticle

Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.

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Instituto Universitario de Enfermedades Tropicalesy Salud Pública de Canarias, Universidad de La Laguna, Avda Francisco Sanchez s/n, Campus de Anchieta, 38271 La Laguna Tenerife, Islas Canarias, Espana
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Laboratoire Matériaux-Molécules et Applications, University of Carthage, La Marsa Tunisia, Tunisia
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Instituto Universitario de Bio-Orgánica Antonio González, Departamento de Química Orgánica, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, Islas Canarias, Espana
*
Authors to whom correspondence should be addressed.
Pathogens 2019, 8(3), 130; https://doi.org/10.3390/pathogens8030130
Received: 1 August 2019 / Revised: 20 August 2019 / Accepted: 21 August 2019 / Published: 23 August 2019
(This article belongs to the Special Issue Emerging Parasitic Protozoa)
The current chemotherapy of Acanthamoeba keratitis relies on few drugs with low potential and limited efficacy, for all this there is an urgent need to identify new classes of anti-Acanthamoeba agents. In this regard, natural products play an important role in overcoming the current need and medicinal chemistry of natural products represents an attractive approach for the discovery and development of new agents. Ursolic acid, a natural pentacyclic triterpenoid compound, possesses a broad spectrum of activities including anti-Acanthamoeba. Herein, we report on the development by chemical transformation of an ursolic acid-based series of seven compounds (2–8), one of them reported for the first time. The structure-activity relationship (SAR) analysis of their anti-Acanthamoeba activity revealed that acylation/ether formation or oxidation enhances their biological profile, suggesting that the hydrophobic moiety contributes to activity, presumably by increasing the affinity and/or cell membrane permeability. These ursolic acid derivatives highlight the potential of this source as a good base for the development of novel therapeutic agents against Acanthamoeba infections. View Full-Text
Keywords: ursolic acid derivatives; Acanthamoeba; chemotherapy; programmed cell death ursolic acid derivatives; Acanthamoeba; chemotherapy; programmed cell death
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Sifaoui, I.; Rodríguez-Expósito, R.L.; Reyes-Batlle, M.; Rizo-Liendo, A.; Piñero, J.E.; Bazzocchi, I.L.; Lorenzo-Morales, J.; Jiménez, I.A. Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.. Pathogens 2019, 8, 130.

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