Design, Synthesis and Evaluation of Novel 2-(Aminoalkyl)-isoindoline-1,3-dione Derivatives as Dual-Binding Site Acetylcholinesterase Inhibitors was written by Ignasik, Michalina;Bajda, Marek;Guzior, Natalia;Prinz, Michaela;Holzgrabe, Ulrike;Malawska, Barbara. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2012.Electric Literature of C13H14BrNO2 This article mentions the following:
A new series of 2-(diethylaminoalkyl)-isoindoline-1,3-dione derivatives intended as dual binding site cholinesterase inhibitors were designed using mol. modeling and evaluated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and the formation of the β-amyloid (Aβ) plaques. For AChE inhibitory activity, the spectrophotometric method of Ellman and the electrophoretically mediated microanal. assay were used, giving good results. Most of the synthesized compounds had AChE inhibitory activity with IC50 values ranging from IC50 = 0.9 to 19.5 μM and weak Aβ anti-aggregation inhibitory activity. These results support the outcome of docking studies which tested compounds targeting both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. The most promising selective AChE inhibitors are compounds 10 (IC50 = 1.2 μM) and 11 (IC50 = 1.1 μM), with 6-7 methylene chains, which also inhibit Aβ fibril formation. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Electric Literature of C13H14BrNO2).
N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Electric Literature of C13H14BrNO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary