In 2010,Young, Brandon M.; Hyatt, Janice L.; Bouck, David C.; Chen, Taosheng; Hanumesh, Parimala; Price, Jeanine; Boyd, Vincent A.; Potter, Philip M.; Webb, Thomas R. published 《Structure-Activity Relationships of Substituted 1-Pyridyl-2-phenyl-1,2-ethanediones: Potent, Selective Carboxylesterase Inhibitors》.Journal of Medicinal Chemistry published the findings.Synthetic Route of C5H5BrN2 The information in the text is summarized as follows:
Inhibition of intestinal carboxylesterases may allow modification of the pharmacokinetics/pharmacodynamic profile of existing drugs by altering half-life or toxicity. Since previously identified diarylethane-1,2-dione inhibitors are decidedly hydrophobic, a modified dione scaffold was designed and elaborated into a >300 member library, which was subsequently screened to establish the SAR for esterase inhibition. This allowed the identification of single digit nanomolar hiCE inhibitors that showed improvement in selectivity and measured solubility In the experiment, the researchers used 6-Bromopyridin-3-amine(cas: 13534-97-9Synthetic Route of C5H5BrN2)
6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Synthetic Route of C5H5BrN2