2-Mercaptomethyl-thiazolidines use conserved aromatic–S interactions to achieve broad-range inhibition of metallo-β-lactamases
María-Agustina Rossi, V. Rodríguez Martínez, Philip Hinchliffe, María F. Mojica, Valerie Castillo, Diego M. Moreno, Ryan Smith, Brad Spellberg, George L. Drusano, Claudia Banchio, Robert A. Bonomo, James Spencer, Alejandro J. Vila, Graciela Mahler
Abstract
, and restore carbapenem potency against clinical isolates expressing B1 MBLs. Based on their inhibitory profile and lack of eukaryotic cell toxicity, MMTZs represent a promising scaffold for MBL inhibitor development. These results also suggest sulphur-π interactions can be exploited for general ligand design in medicinal chemistry.
Topics & Concepts
ChemistryCombinatorial chemistryRange (aeronautics)StereochemistryMaterials scienceComposite materialPhenothiazines and Benzothiazines Synthesis and ActivitiesSynthesis and Catalytic ReactionsPneumocystis jirovecii pneumonia detection and treatment