101292-95-9Relevant articles and documents
Aqueous metal-free hydrothiolation of enamides and enecarbamates
Barman, Eliezer,Hourezadeh,Lim, Daniel
supporting information, (2019/08/01)
An efficient and metal-free, anti-Markovnikov selective, hydrothioaltion reaction of enamides and enecarbamates in an aqueous medium is presented. This protocol is operationally simple, mild, and atom-economical. This process provides access to thioethers
Synthesis and biological evaluation of analogues of a novel inhibitor of β-amyloid secretion
Chakrabarti, Enakshi,Ghosh, Subrata,Sadhukhan, Sushabhan,Sayre, Lawrence,Tochtrop, Gregory P.,Smith, Jonathan D.
experimental part, p. 5302 - 5319 (2010/10/20)
A drug library of 17200 compounds was screened to select small molecules that inhibit the secretion of amyloid β peptide (Aβ), the major component of Alzheimer disease senile plaques, from a human neuronal cell line. Twenty-nine hits were validated that decreased Aβ secretion by >40% at 10 μM, for a 0.17% hit rate. A lead hit was selected for further study based on its activity and low cytotoxicity, and it was found to inhibit Aβ secretion through activation of the α-secretase pathway. Twenty-four commercially available and 53 synthesized analogues were analyzed for activity. Selected analogues were evaluated for biological stability by incubation with hepatoma cells and for transcellular permeability using Caco-2 cell monolayers. The analogue with the best permeability was evaluated in 2-month old amyloid precursor protein transgenic mice and found to acutely reduce cerebral Aβ levels by 40% after a single iv administration.
