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Can I read 4-Amino-1,2,4-triazole-3-thione as a Promising Scaffold for the Inhibition of Serine and Metallo- β -Lactamases on EtoBox?
4-Amino-1,2,4-triazole-3-thione as a Promising Scaffold for the Inhibition of Serine and Metallo- β -Lactamases by Linciano, Pasquale; Gianquinto, Eleonora; Montanari, Martina; Maso, Lorenzo; Bellio, Pierangelo; Cebrián-Sastre, Esmeralda; Celenza, Giuseppe; Blázquez, JesÃos; Cendron, Laura; Spyrakis, Francesca; Tondi, Donatella is a Medicine article available to read on EtoBox.
What is 4-Amino-1,2,4-triazole-3-thione as a Promising Scaffold for the Inhibition of Serine and Metallo- β -Lactamases about?
The emergence of bacteria that co-express serine- and metallo- carbapenemases is a threat to the efficacy of the available __β__-lactam antibiotic armamentarium. The 4-amino-1,2,4-triazole-3-thione scaffold has been selected as the starting chemical moiety in the design of a small library of __β__-Lactamase inhibitors (BLIs) with extended activity profiles. The synthesised compounds have been validated in vitro against class A serine __β−__Lactamase (SBLs) KPC-2 and class B1 metallo __β−__Lactamases (MBLs) VIM-1 and IMP-1. Of the synthesised derivatives, four compounds showed cross-class micromolar inhibition potency and therefore underwent __in silico__ analyses to elucidate their binding mode within the catalytic pockets of serine- and metallo-BLs. Moreover, several members of the synthesised library have been evaluated, in combination with meropenem (MEM), against clinical strains that overexpress BLs for their ability to synergise carbapenems.
Who reads 4-Amino-1,2,4-triazole-3-thione as a Promising Scaffold for the Inhibition of Serine and Metallo- β -Lactamases?
It is typically read by researchers, students, and practitioners in Medicine.
- Author
- Linciano, Pasquale; Gianquinto, Eleonora; Montanari, Martina; Maso, Lorenzo; Bellio, Pierangelo; Cebrián-Sastre, Esmeralda; Celenza, Giuseppe; Blázquez, JesÃos; Cendron, Laura; Spyrakis, Francesca; Tondi, Donatella
- Publisher
- MDPI AG; Multidisciplinary Digital Publishing Institute (MDPI); Basel: MDPI Molecular Diversity Preservation International, 2004- (ISSN 1424-8247)
- Published
- 2020
- Language
- EN
- Field
- Medicine (Life Sciences)