N-Thio-β-lactams targeting L,D-transpeptidase-2, with activity against drug-resistant strains of Mycobacterium tuberculosis
Giulia Martelli, Tomás Bohn Pessatti, Eva Maria Steiner, Martina Cirillo, Caso Carolina, Francesco Bisognin, Michael Landreh, Paola Dal Monte, Daria Giacomini, R. Schnell
Abstract
. The resulting stable adducts lead to a long-term inactivation of the target protein. Finally, the candidates were evaluated in vitro against a drug-susceptible and multidrug-resistant clinical isolates of M. tuberculosis, confirming the antimycobacterial effect of these novel compounds.
Topics & Concepts
Mycobacterium tuberculosisTuberculosisAntimycobacterialChemistryThio-MicrobiologyLigand (biochemistry)AntimicrobialDrug resistanceLactamLigand efficiencyCombinatorial chemistryBiologyStereochemistryMedicineBiochemistryReceptorPathologySynthesis of β-Lactam CompoundsPneumocystis jirovecii pneumonia detection and treatmentCancer therapeutics and mechanisms