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

被引:0
|
作者
Kocharov, S. L. [1 ,2 ]
Panosyan, H. A. [1 ,3 ]
Mirzoyan, L. S. [1 ,2 ]
Nazaryan, I. M. [1 ,2 ]
Paronikyan, R. G. [1 ,2 ]
机构
[1] Natl Acad Sci Armenia, Sci & Technol Ctr Organ & Pharmacol Chem, 26 Azatutyan Prosp, Yerevan 0014, Armenia
[2] AL Mnjoyan Inst Fine Organ Chem, Yerevan, Armenia
[3] Mol Struct Res Ctr, Yerevan, Armenia
关键词
beta-cycloketols; alpha; omega-bis(4-formylphenoxy)alkanes; Knoevenagel condensation; diaminoalkanes; dialdehydes; neurotropic activity; ANTICONVULSANT ACTION; P-ISOPROPOXYPHENYLSUCCINIMIDE; ANTIEPILEPTIC DRUGS; CHEMICAL-STRUCTURE; VALPROATE; RATS;
D O I
10.1007/s11094-024-03200-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Two types of known and new derivatives of substituted beta-cycloketols were synthesized; characterized using IR, PMR, and C-13 NMR spectroscopy; and tested for neurotropic activity. Bioscreening of the compounds was performed. A study of the neurotropic properties of the synthesized new beta-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.
引用
收藏
页码:730 / 737
页数:8
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