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Título: | Symmetry Complementarity-Guided Design of Anthrax Toxin Inhibitors Based on β-Cyclodextrin: Synthesis and Relative Activities of Face-Selective Functionalized Polycationic Clusters |
Autor: | Díaz Moscoso, Alejandro CSIC ORCID ; Méndez-Ardoy, Alejandro CSIC ORCID; Ortega-Caballero, Fernando; Benito, Juan M. CSIC ORCID CVN ; Ortiz-Mellet, Carmen; Defaye, Jacques; Robinson, Tanisha M.; Yohannes, Adiamseged; Karginov, Vladimir A.; García Fernández, José Manuel CSIC ORCID | Palabras clave: | Anthrax Click chemistry Cyclodextrins Symmetry complementary Toxin inhibitors |
Fecha de publicación: | 7-dic-2010 | Editor: | Wiley-VCH | Citación: | ChemMedChem 6(1): 181-192 (2011) | Resumen: | Three new series of potential anthrax toxin inhibitors based on the β-cyclodextrin (βCD) scaffold were developed by exploiting face-selective CuI-catalyzed azide–alkyne 1,3-cycloadditions, amine–isothiocyanate coupling, and allyl group hydroboration–oxidation/hydroxy → amine replacement reactions. The molecular design follows the “symmetry–complementarity” concept between homogeneously functionalized polycationic βCD derivatives and protective antigen (PA), a component of anthrax toxin known to form C7-symmetric pores on the cell membrane used by lethal and edema factors to gain access to the cytosol. The synthesis and antitoxin activity of a collection of βCD derivatives differing in the number, arrangement, and face location of the cationic elements are reported herein. These results set the basis for a structure–activity relationship development program of new candidates to combat the anthrax threat. | Descripción: | 12 páginas, 3 figuras, 1 tabla, 4 esquemas. | Versión del editor: | http://dx.doi.org/10.1002/cmdc.201000419 | URI: | http://hdl.handle.net/10261/37025 | DOI: | 10.1002/cmdc.201000419 | ISSN: | 1860-7179 | E-ISSN: | 1860-7187 |
Aparece en las colecciones: | (IIQ) Artículos |
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