Synthesis and neurotropic activity of the derivatives of fused triazolo[4,3-c]- and triazolo[1,5-c]pyrimidines

被引：4

作者：

Paronikyan, E. G. ^{[1
]}

Dashyana, Sh Sh ^{[1
]}

Paronikyan, R. G. ^{[1
]}

Dzhagatspanyan, I. A. ^{[1
]}

Nazaryan, I. M. ^{[1
]}

Akopyan, A. G. ^{[1
]}

Minasyan, N. S. ^{[2
]}

机构：

[1] Natl Acad Sci Armenia, Mndzhoyan Inst Fine Organ Chem, Sci & Technol Ctr Organ & Pharmaceut Chem, Yerevan 0014, Armenia

[2] Natl Acad Sci Armenia, Mol Struct Res Ctr, Sci & Technol Ctr Organ & Pharmaceut Chem, Yerevan 0014, Armenia

来源：

RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY | 2017年 / 43卷 / 05期

关键词：

triazolo[4,3-c]- and triazolo[1,5-c]pyrimidines; Dimroth rearrangement; neurotropic activity; anticonvulsant effect; MICE;

D O I：

10.1134/S1068162017040070

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The methods for preparation of fused triazolo[4,3-c]- and triazolo[1,5-c]pyrimidines were developed. The Dimroth rearrangement of these systems was studied. Pharmacological investigation of the synthesized compounds was conducted in known tests, such as antagonism with subcutaneous administration of corazole and the open-field test. The rotating rod method was used to assess the neurotoxicity. Neurotropic properties were found in many derivatives of triazolopyrimidine. They, like diazepam, prevent the occurrence of clonic twitching and corazole-induced clonic convulsions in animals. All selected compounds as well as diazepam exhibit an anxiolytic effect.

引用

页码：595 / 603

页数：9

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