V
Valerie Castillo
Researcher at University of the Republic
Publications - 8
Citations - 254
Valerie Castillo is an academic researcher from University of the Republic. The author has contributed to research in topics: Iminium & Dynamic combinatorial chemistry. The author has an hindex of 5, co-authored 7 publications receiving 189 citations.
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Journal ArticleDOI
Cross-class metallo-β-lactamase inhibition by bisthiazolidines reveals multiple binding modes
Philip Hinchliffe,Mariano M. González,Maria F. Mojica,Javier M. González,Valerie Castillo,Cecilia Saiz,Magda Kosmopoulou,Catherine L. Tooke,Leticia I. Llarrull,Graciela Mahler,Robert A. Bonomo,Alejandro J. Vila,James Spencer +12 more
TL;DR: A series of small compounds, bisthiazolidines, which act as inhibitors of all MBL types, restoring the efficacy of currently used antibiotics against resistant bacterial strains producing different MBLs are shown.
Journal ArticleDOI
Bisthiazolidines: A Substrate-Mimicking Scaffold as an Inhibitor of the NDM-1 Carbapenemase
Mariano M. González,Magda Kosmopoulou,Maria F. Mojica,Valerie Castillo,Philip Hinchliffe,Ilaria Pettinati,Jürgen Brem,Christopher J. Schofield,Graciela Mahler,Robert A. Bonomo,Leticia I. Llarrull,James Spencer,Alejandro J. Vila +12 more
TL;DR: Inspired by known interactions of MBLs with β-lactams, four BTZs are designed that behave as in vitro NDM-1 inhibitors with Ki values in the low micromolar range and restore the antibacterial activity of imipenem.
Journal ArticleDOI
Discovering Echinococcus granulosus thioredoxin glutathione reductase inhibitors through site-specific dynamic combinatorial chemistry
Cecilia Saiz,Valerie Castillo,Pablo Fontán,Mariana Bonilla,Gustavo Salinas,Alejandra Rodríguez-Haralambides,Graciela Mahler +6 more
TL;DR: The results validate the use of DCL for targeting thiol-disulfide oxido-reductases and use of 5-thio-2-nitrobenzoic acid as a non-covalent anchor fragment in a DCL templated by E. granulosus TGR.
Journal ArticleDOI
2-Mercaptomethyl-thiazolidines use conserved aromatic–S interactions to achieve broad-range inhibition of metallo-β-lactamases
Maria Agustina Rossi,Verónica Martínez,Philip Hinchliffe,Maria F. Mojica,Maria F. Mojica,Maria F. Mojica,Valerie Castillo,Diego M. Moreno,Diego M. Moreno,Ryan Smith,Brad Spellberg,George L. Drusano,Claudia Banchio,Claudia Banchio,Robert A. Bonomo,James Spencer,Alejandro J. Vila,Alejandro J. Vila,Graciela Mahler +18 more
TL;DR: A series of 2-mercaptomethyl-thiazolidines (MMTZs) designed to replicate MBL interactions with reaction intermediates or hydrolysis products are synthesised and suggest sulphur–π interactions can be exploited for general ligand design in medicinal chemistry.
Journal ArticleDOI
Imine Domino Reactions Generate Novel Scaffolds: Fused Bisthiazolidines or Bisthiiranes
TL;DR: In this article, β-Aminothiols (II) and (V) react with 2-mercaptoacetaldehyde to generate iminium ions which cyclize to novel fused bisthiazolidines.