@misc{10481/107604,
year = {2020},
month = {6},
url = {https://hdl.handle.net/10481/107604},
abstract = {Leishmania (L.) infantum causes visceral, cutaneous, and mucosal leishmaniasis in humans and canine leishmaniasis in dogs. Herein, we describe that O-alkyl hydroxamate derivatives displayed potent and selective in vitro activity against the amastigote stage of L. infantum while no activity was observed against promastigotes. Compound 5 showed potent in vivo activity against L. infantum. Moreover, the combination of compound 5 supported on gold nanoparticles and meglumine antimoniate was also effective in vivo and improved the activity of these compounds compared to that of the individual treatment. Docking studies showed that compound 5 did not reach highly conserved pocket C and established interactions with the semiconserved residues V44, A45, R242, and E243 in pocket A of LiSIR2rp1. The surface space determined by these four amino acids is not conserved in human sirtuins. Compound 5 represents a new class of selective ligands with antileishmanial activity.},
organization = {This research was supported by Project P06-CTS-01407 from the Junta de Andalucía (Spain), Project GREIB.PT-2010-10 from the Universidad de Granada (Spain), and Project 20F12/7 from the Universidad de Granada (Spain).},
publisher = {American Chemical Society},
keywords = {Metal nanoparticles},
keywords = {Nanoparticles},
keywords = {Parasites},
keywords = {Peptides and proteins},
keywords = {Redox reactions},
title = {O-Alkyl Hydroxamates Display Potent and Selective Antileishmanial Activity},
doi = {https://doi.org/10.1021/acs.jmedchem.9b02016},
author = {Corpas-López, Victoriano and Tabraue-Chavez, Mavys and Sixto-López, Yudibeth and Panadero-Fajardo, Sonia and Alves de Lima Franco, Fernando and Domínguez Seglar, José Francisco and Morillas Márquez, Francisco and Franco Montalbán, Francisco and Díaz Gavilán, Mónica and Correa-Basurto, José and López-Viota, Julián and López-Viota Gallardo, Margarita and Pérez del Palacio, José and de la Cruz, Mercedes and de Pedro, Nuria and Martín Sánchez, Joaquina and Gómez Vidal, José Antonio},
}