Nicotinamide and nicotinonitrile derivatives containing a C
5
–C
7
-cycloalkane ring fused to the C
4
–C
5
bond were synthesized via Knoevenagel condensation, nucleophilic vinylic substitution (S
N
...Vin), and alkylation. The structure of (1-amino-5-phenyl-5,6,7,8-tetrahydrothieno2,3-
c
isoquinolin-2-yl)(phenyl)methanone was determined by X-ray analysis.
We studied the effect of a new cyanine dye containing selenium and tellurium on acetylcholinesterase activity in synaptic membrane in rat brain. The cyanine dye dose-dependently inhibits activity of ...this enzyme, and the concentration of half-maximal inhibition of acetylcholinesterase activity was 20.46 μM. The cyanine dye instantly inhibits the enzyme; the degree of inhibition depends on acetylthiocholine concentration: the lower is acetylthiocholine concentration, the higher is the degree of inhibition. On the Lineweaver—Burk plot, the concentration dependence curves of acetylcholinesterase with and without cyanine dye intersect in one point on the abscissa axis. In this case, the cyanine dye reduces the maximum inhibition rate (V
max
) and does not affect Michaelis constant (K
m
). The calculated inhibition constant K
i
for the cyanine dye is 7.74 μM. Thus, the cyanine dye is a non-competitive inhibitor of acetylcholinesterase.
New reagents for the synthesis of substituted selenazoles, 3-amino-
N
-cyclopropyl-3-selanylidenepropanamide and methyl 3-amino-3-selanylidenepropanoate, were obtained by reactions of 2-cyano-
N
...-cyclopropylacetamide and methyl 2-cyanoacetate with hydrogen selenide. The structure of the products was confirmed by IR,
1
H and
13
C NMR, and mass spectra.
A new method for the synthesis of 6,7-dimethoxy-3,4-dihydroisoquinoline based on the reaction of 2-(3,4-dimethoxyphenyl)ethan-1-amine (homoveratrylamine) with aliphatic nitro compounds in ...polyphosphoric acid (PPA) was developed.
A novel
one-pot
method based on the sequence of the Fisher reaction between nitroacetophenone and phenylhydrazines, the reduction with metallic tin directly in polyphosphoric acid, and acylation has ...been developed for the synthesis of indoloquinolines. The obtained indolo-3,2-
c
quinolines are precursors of the analogs of isocryptolepine alkaloid.
A new method for synthesizing 11
H
-indolo3,2-
c
quinolines by SnCl
4
-catalyzed intramolecular electrophilic amination of 2-arylindole-3-carbaldehyde
O
-acetyl oximes was developed.
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