S. L. Kocharov, H. A. Panosyan, L. S. Mirzoyan, I. M. Nazaryan, R. G. Paronikyan
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Synthesis and Evaluation of the Neurotropic Activity of New β-Cycloketol Derivatives
Two types of known and new derivatives of substituted β-cycloketols were synthesized; characterized using IR, PMR, and 13C NMR spectroscopy; and tested for neurotropic activity. Bioscreening of the compounds was performed. A study of the neurotropic properties of the synthesized new β-cycloketol derivatives revealed that some of them exhibited a pronounced anticonvulsant effect as antagonism of corazol. The compounds were superior in anticonvulsant activity to the well-known drug ethosuximide but inferior to diazepam. Like ethosuximide, the studied compounds did not exhibit central muscle relaxant activity at anticonvulsant doses, unlike diazepam. However, they exhibited psychotropic effects, e.g., pronounced anxiolytic, antidepressant, and activating behavior. The results showed that further searching for neurotropic properties in new polyfunctional cycloketol derivatives was advisable.
期刊介绍:
Pharmaceutical Chemistry Journal is a monthly publication devoted to scientific and technical research on the creation of new drugs and the improvement of manufacturing technology of drugs and intermediates. International contributors cover the entire spectrum of new drug research, including:
methods of synthesis;
results of pharmacological, toxicological, and biochemical studies;
investigation of structure - activity relationships in prediction of new compounds;
methods and technical facilities used; and
problems associated with the development of ecologically safe and economically feasible methods of industrial production.
In addition, analytical reviews of the international literature in the field provide coverage of the most recent developments around the world.
Pharmaceutical Chemistry Journal is a translation of the Russian journal Khimiko-Farmatsevticheskii Zhurnal. The Russian Volume Year is published in English from April.
All articles are peer-reviewed.