《Discovery of Novel Inhibitors of LpxC Displaying Potent in Vitro Activity against Gram-Negative Bacteria》 was written by Surivet, Jean-Philippe; Panchaud, Philippe; Specklin, Jean-Luc; Diethelm, Stefan; Blumstein, Anne-Catherine; Gauvin, Jean-Christophe; Jacob, Loic; Masse, Florence; Mathieu, Gaelle; Mirre, Azely; Schmitt, Christine; Lange, Roland; Tidten-Luksch, Naomi; Gnerre, Carmela; Seeland, Swen; Herrmann, Charlyse; Seiler, Peter; Enderlin-Paput, Michel; Mac Sweeney, Aengus; Wicki, Micha; Hubschwerlen, Christian; Ritz, Daniel; Rueedi, Georg. COA of Formula: C4H7NO2S And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:
UDP-3-O-((R)-3-hydroxymyristoyl)-N-glucosamine deacetylase (LpxC) is as an attractive target for the discovery and development of novel antibacterial drugs to address the critical medical need created by multidrug resistant Gram-neg. bacteria. By using a scaffold hopping approach on a known family of methylsulfone hydroxamate LpxC inhibitors, several hit series eliciting potent antibacterial activities against Enterobacteriaceae and Pseudomonas aeruginosa were identified. Subsequent hit-to-lead optimization, using cocrystal structures of inhibitors bound to Pseudomonas aeruginosa LpxC as guides, resulted in the discovery of multiple chem. series based on (i) isoindolin-1-ones, (ii) 4,5-dihydro-6H-thieno[2,3-c]pyrrol-6-ones, and (iii) 1,2-dihydro-3H-pyrrolo[1,2-c]imidazole-3-ones. Synthetic methods, antibacterial activities and relative binding affinities, as well as physicochem. properties that allowed compound prioritization are presented. Finally, in vivo properties of lead mols. which belong to the most promising pyrrolo-imidazolone series, such as I, are discussed. In the experiment, the researchers used many compounds, for example, Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1COA of Formula: C4H7NO2S)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.COA of Formula: C4H7NO2S
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