《Mycobacterium tuberculosis Decaprenylphosphoryl-β-D-ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity》 was written by Borthwick, Jennifer A.; Alemparte, Carlos; Wall, Ian; Whitehurst, Benjamin C.; Argyrou, Argyrides; Burley, Glenn; de Dios-Anton, Paco; Guijarro, Laura; Monteiro, Maria Candida; Ortega, Fatima; Suckling, Colin J.; Pichel, Julia Castro; Cacho, Monica; Young, Robert J.. Product Details of 1193-21-1 And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:
Decaprenylphosphoryl-β-D-ribose 2′-epimerase (DprE1) is an essential enzyme in Mycobacterium tuberculosis and has recently been studied as a potential drug target, with inhibitors progressing to clin. studies. Here we describe the identification of a novel series of morpholino-pyrimidine DprE1 inhibitors. These were derived from a phenotypic high-throughput screening (HTS) hit with suboptimal physicochem. properties. Optimization strategies included scaffold-hopping, synthesis, and evaluation of fragments of the lead compounds and property-focused optimization. The resulting optimized compounds had much improved physicochem. properties and maintained enzyme and cellular potency. These mols. demonstrated potent efficacy in an in vivo tuberculosis murine infection model. After reading the article, we found that the author used 4,6-Dichloropyrimidine(cas: 1193-21-1Product Details of 1193-21-1)
4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Product Details of 1193-21-1
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia