On July 5, 2021, Romero, Eugenie; Oueslati, Saoussen; Benchekroun, Mohamed; D′Hollander, Agathe C. A.; Ventre, Sandrine; Vijayakumar, Kamsana; Minard, Corinne; Exilie, Cynthia; Tlili, Linda; Retailleau, Pascal; Zavala, Agustin; Elisee, Eddy; Selwa, Edithe; Nguyen, Laetitia A.; Pruvost, Alain; Naas, Thierry; Iorga, Bogdan I.; Dodd, Robert H.; Cariou, Kevin published an article.Related Products of 141940-37-6 The title of the article was Azetidinimines as a novel series of non-covalent broad-spectrum inhibitors of β-lactamases with submicromolar activities against carbapenemases KPC-2 (class A), NDM-1 (class B) and OXA-48 (class D). And the article contained the following:
The occurrence of resistances in Gram neg. bacteria is steadily increasing to reach extremely worrying levels and one of the main causes of resistance is the massive spread of very efficient β-lactamases which render most β-lactam antibiotics useless. Herein, we report the development of a series of imino-analogs of β-lactams (namely azetidinimines) as efficient non-covalent inhibitors of β-lactamases. Despite the structural and mechanistic differences between serine-β-lactamases KPC-2 and OXA-48 and metallo-β-lactamase NDM-1, all three enzymes can be inhibited at a submicromolar level by compound 7dfm (I), which can also repotentiate imipenem against a resistant strain of Escherichia coli expressing NDM-1. We show that 7dfm can efficiently inhibit not only the three main clin.-relevant carbapenemases of Ambler classes A (KPC-2), B (NDM-1) and D (OXA-48) with Ki′s below 0.3 μM, but also the cephalosporinase CMY-2 (class C, 86% inhibition at 10 μM). Our results pave the way for the development of a new structurally original family of non-covalent broad-spectrum inhibitors of β-lactamases. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Related Products of 141940-37-6
The Article related to azetidinimine noncovalent beta lactamase inhibitor, azetidinimines, bacterial resistance, carbapenemase inhibitors, kpc-2, ndm-1, oxa-48, ynamides, Placeholder for records without volume info and other aspects.Related Products of 141940-37-6
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics