Studies in the Thiamorpholine Series. III. Derivatives of Thiamorpholine-3,5-dicarboxylic Acid

1940 ◽  
Vol 62 (6) ◽  
pp. 1615-1616 ◽  
Author(s):  
Edwin O. Hook ◽  
Helen I. Miner ◽  
Robert D. Coghill
2020 ◽  
Vol 6 (4) ◽  
pp. 51-57
Author(s):  
Ekaterina E. Yakovleva ◽  
Eugeny R. Bychkov ◽  
Maria M. Brusina ◽  
Levon B. Piotrovsky ◽  
Petr D. Shabanov

Objective: To study the antiparkinsonian activity of new 1,2-substituted imidazole-4,5-dicarboxylic acids in dopaminergic transmission suppression tests in mice and rats. Materials and methods: On a model of reserpine extrapyramidal disorders, the derivatives of imidazole-dicarboxylic acids (IEM2258, IEM2248, IEM2247) were injected into the lateral brain ventricles of the mice 30 minutes after injecting reserpine at the doses of 0.1–0.5 mmol. Locomotor activity was analyzed in the Open-field test 2 hours later. In the catalepsy model, the studied agents were injected, using a pre-implanted cannula, with a simultaneous intraperitoneal injection of haloperidol. The severity of catalepsy was assessed with the Morpurgo method. Amantadine was used as a comparator drug in all the tests. Results: It was shown that IEM2258 significantly increased the main indicators of locomotor activity in the Open-field test at all the studied doses. The value of the antiparkinsonian effect of IEM2258 at doses of 0.4–0.5 mmol significantly exceeded that of amantadine. The antiparkinsonian effect of IEM2247 was maximally expressed and was significantly different from those in the control and comparator group at doses of 0.2 and 0.3 mmol. For all the experimental groups, a significant decrease in the manifestations of catalepsy in comparison with control indexes was determined. Discussion: The results made it possible to suggest the involvement of imidazole-4,5-dicarboxylic acids derivatives in the process of experimental improvement of dopaminergic neuromodulation and efficiency in animals. Conclusion: The data showed a significant dose-dependent antiparkinsonian activity of new imidazole-4,5-dicarboxylic acid derivatives, which makes it promising to develop these agents and to further search for effective and safe antiparkinsonian drugs in this pharmacological class. Graphical abstract


1942 ◽  
Vol 64 (7) ◽  
pp. 1572-1576 ◽  
Author(s):  
Maurice L. Moore ◽  
Charles S. Miller

1949 ◽  
Vol 27b (5) ◽  
pp. 437-461 ◽  
Author(s):  
Y. Hirshberg ◽  
R. Norman Jones

The ultraviolet absorption spectra of a variety of naphthalene compounds containing phenyl and carboxy substituents are described. The majority of the compounds contain either the naphthalene-1,2-dicarboxylic acid anhydride or the naphthalene-2,3-dicarboxylic acid anhydride ring systems. It is shown that in ethanolic solution the spectra of these anhydrides change over a period of a few hours. The spectra of the anhydrides in n-heptane or dioxane solution do not change on standing. The effects of the various substituents are discussed in terms of steric inhibition of resonance and of antagonistic and reinforcing actions of the substituents, dependent on the position of substitution. The significance of these data are considered in relation to the general problem of the interpretation of the ultraviolet absorption spectra of complex molecules.


ChemInform ◽  
2010 ◽  
Vol 28 (38) ◽  
pp. no-no
Author(s):  
R. G. KOSTYANOVSKY ◽  
I. I. CHERVIN ◽  
G. K. KADORKINA ◽  
K. N. MAKAROV ◽  
L. T. LANTZEVA ◽  
...  

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