This invention discloses chemical compounds having the following structural formula ##SPC1## Wherein X is chlorine or fluorine; n is an integer from 1 to 3; and Y is chlorine, bromine or fluorine. The compounds of the above description are useful as insecticides.
An efficient strategy for the para-selective borylation of aromatic esters is described. For achieving high para-selectivity, a new catalytic system has been developed modifying the core structure of the bipyridine. It has been proposed that the L-shaped ligand is essential to recognize the functionality of the oxygen atom of the ester carbonyl group via noncovalent interaction, which provides an unprecedented
Synthesis and Biological Evaluation of Analogues of a Novel Inhibitor of β-Amyloid Secretion
作者:Enakshi Chakrabarti、Subrata Ghosh、Sushabhan Sadhukhan、Lawrence Sayre、Gregory P. Tochtrop、Jonathan D. Smith
DOI:10.1021/jm100308g
日期:2010.7.22
A drug library of 17200 compounds was screened to select small molecules that inhibit the secretion of amyloid beta peptide (Am, the major component of Alzheimer disease senile plaques, from a human neuronal cell line. Twenty-nine hits were validated that decreased A beta secretion by >40% at 10 mu M, 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 A beta secretion through activation of the alpha-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 A beta levels by 40% after a single iv administration.
WO2007/144327
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Sudborough, Journal of the Chemical Society, 1895, vol. 67, p. 602