- Aqueous metal-free hydrothiolation of enamides and enecarbamates
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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
- Barman, Eliezer,Hourezadeh,Lim, Daniel
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supporting information
(2019/08/01)
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- COMPOSITIONS AND METHODS FOR INHIBITING BETA AMYLOID SECRETION
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A pharmaceutical composition for inhibiting amyloid beta peptide in a subject includes a compound having the formula (I): where M is selected from a substituted or unsubstituted alkyl, halo, alkoxy, aryl, cyclic, or heterocyclic group; p is an integer from 0-3; X1 is a 3-9 atoms in length linker connecting A and B; B is selected from a substituted or unsubstituted aryl, alkoxy or amine group; and a pharmaceutically acceptable salt thereof; and a pharmaceutical carrier.
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Paragraph 0076; 0119
(2013/06/28)
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- Synthesis and biological evaluation of analogues of a novel inhibitor of β-amyloid secretion
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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.
- Chakrabarti, Enakshi,Ghosh, Subrata,Sadhukhan, Sushabhan,Sayre, Lawrence,Tochtrop, Gregory P.,Smith, Jonathan D.
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experimental part
p. 5302 - 5319
(2010/10/20)
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