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

Preparation and Mechanistic Studies of 2-Substituted Bisthiazolidines by Imine Exchange

Autor: Valentina Villamil, Diego Duarte, Nicolás Veiga, Carolina Fontana, Graciela Mahler, Danilo Davyt, Verónica Martínez, Cecilia Saiz

Publikováno v: European Journal of Organic Chemistry. 2020:1084-1092

Bisthiazolidines (BTZ) are bicyclic compounds considered penicillin analogs that inhibit the full range of Metallo-β-Lactamases (MBLs) and potentiate β-lactam activity against resistant bacteria. Herein we present a new methodology to prepare 2-sub

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ec6991545d7f46bd507d6aa554096ec2
https://doi.org/10.1002/ejoc.201901677

A new procedure for thioester deprotection using thioglycolic acid in both homogeneous and heterogeneous phase

Autor: Valentina Villamil, Cecilia Saiz, Graciela Mahler

Publikováno v: Tetrahedron

Classic acetyl thioester protection/deprotection methodologies are widely used in organic synthesis, but deprotection step usually requires harsh conditions not suitable for labile substrates. In this work, a new method for thioester deprotection usi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::853a51dd30e91cb563f4ee24ce5f4fdf
https://doi.org/10.1016/j.tet.2021.132335

Synthesis of bicyclic 1,4-thiazepines as novel anti

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

Publikováno v: Medchemcomm

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=pmid________::c2bebe8943c5350b926a457973fffa9b
https://pubmed.ncbi.nlm.nih.gov/31673311

Cross-class metallo-β-lactamase inhibition by bisthiazolidines reveals multiple binding modes

Autor: Valerie Castillo, Alejandro J. Vila, Graciela Mahler, Javier M. González, Maria F. Mojica, Cecilia Saiz, Magda Kosmopoulou, Mariano M. González, James Spencer, Catherine L. Tooke, Philip Hinchliffe, Robert A. Bonomo, Leticia I. Llarrull

Publikováno v: Hinchliffe, P, Gonzalez, M M, Mojica, M F, Gonzalez, J M, Castillo, V, Saiz, C, Kosmopoulou, M, Tooke, C, Llarrull, L, Mahler, G, Bonomo, R A, Villa, A J & Spencer, J 2016, ' Cross-class metallo-β-lactamase inhibition by bisthiazolidines reveals multiple binding modes ', Proceedings of the National Academy of Sciences of the United States of America, vol. 113, no. 26, pp. E3745-E3754 . https://doi.org/10.1073/pnas.1601368113
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Metallo-β-lactamases (MBLs) hydrolyze almost all β-lactam antibiotics and are unaffected by clinically available β-lactamase inhibitors (βLIs). Active-site architecture divides MBLs into three classes (B1, B2, and B3), complicating development of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68799a23a5f1b0de2ff1b3625c35706a
https://research-information.bris.ac.uk/en/publications/e66e5c86-fd98-4326-9bee-15426e11504f