1078130-52-5Relevant articles and documents
Acylhydrazone Switches: E/Z Stability Reversed by Introduction of Hydrogen Bonds
Lu, Chaocao,Htan, Bu,Ma, Chunmiao,Liao, Rong-Zhen,Gan, Quan
, p. 7046 - 7050 (2018)
We report a series of acylhydrazone-based switches, of which double bond rotation can be stimulated by a pH response. The switches prefer Z rather than E configuration in the ground state because of the intramolecular hydrogen bonding, which was analyzed both thermodynamically and kinetically. Solvation studies show a linear relationship between the isomerization energy in Z/E states (ΔGE/Zo) of the switches and the hydrogen bond basicity scales (β and DN) of the solvent. This solvent effect was also found to be relative to the skeleton of compound, the less shield of hydrogen bond domain the more sensitivity to the solvent environment. By introducing multiple intramolecular hydrogen bonds, the Z isomer completely predominates for compound 4, offering an advantage over a full E/Z isomerization switching.
QUINOLINE AMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 63, (2011/08/03)
The present invention is directed to quinoline amide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.