Synthetic Route of C5H5BrN2On June 7, 2021, Adamek, Rebecca N.; Suire, Caitlin N.; Stokes, Ryjul W.; Brizuela, Monica K.; Cohen, Seth M.; Leissring, Malcolm A. published an article in ChemMedChem. The article was 《Hydroxypyridinethione Inhibitors of Human Insulin-Degrading Enzyme》. The article mentions the following:
Insulin-degrading enzyme (IDE) is a human mononuclear Zn2+-dependent metalloenzyme that is widely regarded as the primary peptidase responsible for insulin degradation Despite its name, IDE is also critically involved in the hydrolysis of several other disparate peptide hormones, including glucagon, amylin, and the amyloid β-protein. As such, the study of IDE inhibition is highly relevant to deciphering the role of IDE in conditions such as type-2 diabetes mellitus and Alzheimer disease. There have been few reported IDE inhibitors, and of these, inhibitors that directly target the active-site Zn2+ ion have yet to be fully explored. In an effort to discover new, zinc-targeting inhibitors of IDE, a library of ∼350 metal-binding pharmacophores was screened against IDE, resulting in the identification of 1-hydroxypyridine-2-thione (1,2-HOPTO) as an effective Zn2+-binding scaffold. Screening a focused library of HOPTO compounds identified 3-sulfonamide derivatives of 1,2-HOPTO as inhibitors of IDE (Ki values of ∼50μM). Further structure-activity relationship studies yielded several thiophene-sulfonamide HOPTO derivatives with good, broad-spectrum activity against IDE that have the potential to be useful pharmacol. tools for future studies of IDE. After reading the article, we found that the author used 2-Bromopyridin-3-amine(cas: 39856-58-1Synthetic Route of C5H5BrN2)
2-Bromopyridin-3-amine(cas: 39856-58-1) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Synthetic Route of C5H5BrN2