Synthesis and Evaluation of the Neurotropic Activity of New β-Cycloketol Derivatives

IF 0.8 4区 医学 Q4 CHEMISTRY, MEDICINAL
S. L. Kocharov, H. A. Panosyan, L. S. Mirzoyan, I. M. Nazaryan, R. G. Paronikyan
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引用次数: 0

Abstract

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.

合成和评估新的β-环酮醇衍生物的神经刺激活性
研究人员合成了两种已知和新的β-取代环酮醇衍生物,利用红外光谱、PMR 光谱和 13C NMR 光谱对其进行了表征,并对其神经活性进行了测试。对化合物进行了生物筛选。对合成的新β-环酮醇衍生物的神经刺激特性进行研究后发现,其中一些衍生物具有明显的抗惊厥作用,可拮抗 corazol。这些化合物的抗惊厥活性优于著名药物乙琥胺,但低于地西泮。与乙琥胺一样,所研究的化合物与地西泮不同,在抗惊厥剂量下不表现出中枢肌肉松弛活性。不过,它们表现出了精神作用,如明显的抗焦虑、抗抑郁和激活行为。研究结果表明,进一步研究新的多官能环酮醇衍生物的神经刺激特性是可取的。
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来源期刊
Pharmaceutical Chemistry Journal
Pharmaceutical Chemistry Journal CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY
CiteScore
1.30
自引率
22.20%
发文量
226
审稿时长
3-8 weeks
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.
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