Thioester deprotection using a biomimetic NCL approach

Autor: Valentina Villamil, Cecilia Saiz, Graciela Mahler

Publikováno v: Frontiers in Chemistry, Vol 10 (2022)

The reversibility of the thiol-thioester linkage has been broadly employed in many fields of biochemistry (lipid synthesis) and chemistry (dynamic combinatorial chemistry and material science). When the transthioesterification is followed by a S-to-N

Externí odkaz: https://doaj.org/article/108ec3ee35104ca39036de4c2213a3a1

2-Mercaptomethyl Thiazolidines (MMTZs) Inhibit All Metallo-β-Lactamase Classes by Maintaining a Conserved Binding Mode

Autor: Valentina Villamil, Maria F. Mojica, Brad Spellberg, Diego M. Moreno, James Spencer, Claudia Banchio, Alejandro J. Vila, Robert A. Bonomo, Verónica Martínez, Graciela Mahler, Philip Hinchliffe, George L. Drusano, Maria-Agustina Rossi

Publikováno v: Repositorio U. El Bosque
Universidad El Bosque
instacron:Universidad El Bosque
Hinchliffe, P, Moreno, D M, Rossi, M-A, Mojica, M F, Martinez, V, Villamil, V, Spellberg, B, Drusano, G L, Banchio, C, Mahler, G, Bonomo, R A & Spencer, J 2021, ' 2-Mercaptomethyl Thiazolidines (MMTZs) Inhibit All Metallo-β-Lactamase Classes by Maintaining a Conserved Binding Mode ', ACS Infectious Diseases, vol. 7, no. 9, pp. 2697-2706 . https://doi.org/10.1021/acsinfecdis.1c00194, https://doi.org/10.1021/acsinfecdis.1c00194
ACS Infect Dis

Metallo-β-lactamase (MBL) production in Gram-negative bacteria is an important contributor to β-lactam antibiotic resistance. Combining β-lactams with β-lactamase inhibitors (BLIs) is a validated route to overcoming resistance, but MBL inhibitors

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca170f33eb191f60adbd8e767b6d3429
https://doi.org/10.1021/acsinfecdis.1c00194

A multiscale approach to predict the binding mode of metallo beta-lactamase inhibitors

Autor: Philip Hinchliffe, Alessandro Pedretti, Graciela Mahler, Franco Vairoletti, James Spencer, Adrian J. Mulholland, Silvia Gervasoni

Publikováno v: Gervasoni, S, Spencer, J, Hinchliffe, P, Pedretti, A, Vairoletti, F, Mahler, G & Mulholland, A J 2022, ' A multiscale approach to predict the binding mode of metallo beta-lactamase inhibitors ', Proteins: Structure, Function, and Bioinformatics, vol. 90, no. 2, pp. 372-384 . https://doi.org/10.1002/prot.26227

Antibiotic resistance is a major threat to global public health. β-lactamases, which catalyze breakdown of β-lactam antibiotics, are a principal cause. Metallo β-lactamases (MBLs) represent a particular challenge because they hydrolyze almost all

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2d74f6ffff90604050aa3ab6688bb20
https://research-information.bris.ac.uk/en/publications/d5ca0473-96c9-4ae8-85b4-6010e30e5c18

Synthesis of bicyclic 1,4-thiazepines as novel anti-Trypanosoma brucei brucei agents

Autor: Jenny Saldaña, Jennifer Meléndrez, Andrea Medeiros, Cecilia Saiz, Jaime Franco, Pablo Fontán, Vojtech Jancik, Graciela Mahler, Marcelo A. Comini, Franco Vairoletti, Carlos Tabarez, Gustavo Salinas

Publikováno v: MedChemComm. 10:1481-1487

1,4-Thiazepines derivatives are pharmacologically important heterocycles with different applications in medicinal chemistry. In the present work, we describe the preparation of new bicyclic thiazolidinyl-1,4-thiazepines 3 by reaction between azadithi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ff4b4faaa41ef58964cb1cd824b2b631
https://doi.org/10.1039/c9md00064j

2-Mercaptomethyl-thiazolidines use conserved aromatic-S interactions to achieve broad-range inhibition of metallo-β-lactamases

Autor: Alejandro J. Vila, Brad Spellberg, Claudia Banchio, Ryan Smith, Diego M. Moreno, Graciela Mahler, Maria Agustina Rossi, Robert A. Bonomo, Valerie Castillo, Philip Hinchliffe, George L. Drusano, Verónica Martínez, James Spencer, Maria F. Mojica

Publikováno v: Repositorio U. El Bosque
Universidad El Bosque
instacron:Universidad El Bosque
Chemical Science
Rossi, M-A, Hinchliffe, P, Spencer, J, Vila, A J & Mahler, G 2021, ' 2-Mercaptomethyl-thiazolidines use conserved aromatic-S interactions to achieve broad-range inhibition of metallo-β-lactamases ', Chemical Science, vol. 12, no. 8, pp. 2898-2908 . https://doi.org/10.1039/d0sc05172a

Infections caused by multidrug resistant (MDR) bacteria are a major public health threat. Carbapenems are among the most potent antimicrobial agents that are commercially available to treat MDR bacteria. Bacterial production of carbapenem-hydrolysing

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7af3d56506ac14afb4b81c0d173416ab