Quality Control of EthylbromofluoroacetateOn November 12, 2020 ,《Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases》 appeared in Journal of Medicinal Chemistry. The author of the article were Durand-Reville, Thomas F.; Comita-Prevoir, Janelle; Zhang, Jing; Wu, Xiaoyun; May-Dracka, Tricia L.; Romero, Jan Antoinette C.; Wu, Frank; Chen, April; Shapiro, Adam B.; Carter, Nicole M.; McLeod, Sarah M.; Giacobbe, Robert A.; Verheijen, Jeroen C.; Lahiri, Sushmita D.; Sacco, Michael D.; Chen, Yu; O’Donnell, John P.; Miller, Alita A.; Mueller, John P.; Tommasi, Ruben A.. The article conveys some information:
Multidrug resistant Gram-neg. bacterial infections are an increasing public health threat due to rapidly rising resistance toward β-lactam antibiotics. The hydrolytic enzymes called β-lactamases are responsible for a large proportion of the resistance phenotype. β-Lactamase inhibitors (BLIs) can be administered in combination with β-lactam antibiotics to negate the action of the β-lactamases, thereby restoring activity of the β-lactam. Newly developed BLIs offer some advantage over older BLIs in terms of enzymic spectrum but are limited to the i.v. route of administration. Reported here is a novel, orally bioavailable diazabicyclooctane (DBO) β-lactamase inhibitor. This new DBO, ETX1317(I), contains an endocyclic carbon-carbon double bond and a fluoroacetate activating group and exhibits broad spectrum activity against class A, C, and D serine β-lactamases. The ester prodrug of ETX1317, ETX0282(II), is orally bioavailable and, in combination with cefpodoxime proxetil, is currently in development as an oral therapy for multidrug resistant and carbapenem-resistant Enterobacterales infections. In the part of experimental materials, we found many familiar compounds, such as Ethylbromofluoroacetate(cas: 401-55-8Quality Control of Ethylbromofluoroacetate)
Ethylbromofluoroacetate(cas: 401-55-8) is a member of organofluorine compounds. Organofluorine compounds, which have carbon-fluorine bonds, show unique features such as high thermal and chemical stability, high surface activity, no light-absorbing ability, high pharmacological effect, and so on. Owing to their specific characters, they are indispensable chemicals for industry and our daily lives.Quality Control of Ethylbromofluoroacetate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary