Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies was written by Soares de Melo, Candice;Singh, Vinayak;Myrick, Alissa;Simelane, Sandile B.;Taylor, Dale;Brunschwig, Christel;Lawrence, Nina;Schnappinger, Dirk;Engelhart, Curtis A.;Kumar, Anuradha;Parish, Tanya;Su, Qin;Myers, Timothy G.;Boshoff, Helena I. M.;Barry, Clifton E. III;Sirgel, Frederick A.;van Helden, Paul D.;Buchanan, Kirsteen I.;Bayliss, Tracy;Green, Simon R.;Ray, Peter C.;Wyatt, Paul G.;Basarab, Gregory S.;Eyermann, Charles J.;Chibale, Kelly;Ghorpade, Sandeep R.. And the article was included in Journal of Medicinal Chemistry in 2021.Formula: C3H9NO The following contents are mentioned in the article:
Phenotypic screening of a Medicines for Malaria Venture compound library against Mycobacterium tuberculosis (Mtb) identified a cluster of pan-active 2-pyrazolylpyrimidinones. The biol. triage of these actives using various tool strains of Mtb suggested a novel mechanism of action. The compounds were bactericidal against replicating Mtb and retained potency against clin. isolates of Mtb. Although selected MmpL3 mutant strains of Mtb showed resistance to these compounds, there was no shift in the min. inhibitory concentration (MIC) against a mmpL3 hypomorph, suggesting mutations in MmpL3 as a possible resistance mechanism for the compounds but not necessarily as the target. RNA transcriptional profiling and the checkerboard board 2D-MIC assay in the presence of varying concentrations of ferrous salt indicated perturbation of the Fe-homeostasis by the compounds Structure-activity relationship studies identified potent compounds with good physicochem. properties and in vitro microsomal metabolic stability with moderate selectivity over cytotoxicity against mammalian cell lines. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Formula: C3H9NO).
2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is γ-valerolactone.Formula: C3H9NO
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem