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

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 administratio...

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Published inRussian journal of bioorganic chemistry Vol. 43; no. 5; pp. 595 - 603
Main Authors Paronikyan, E. G., Dashyan, Sh. Sh, Paronikyan, R. G., Dzhagatspanyan, I. A., Nazaryan, I. M., Akopyan, A. G., Minasyan, N. S.
Format Journal Article
LanguageEnglish
Published Moscow Pleiades Publishing 01.09.2017
Springer Nature B.V
Subjects
Biochemistry
Biomedical and Life Sciences
Biomedicine
Bioorganic Chemistry
Convulsions
Derivatives
Life Sciences
Organic Chemistry
Pharmacology
Pyrimidines
Test procedures
Twitching
neurotropic activity
Dimroth rearrangement
pyrimidines
anticonvulsant effect
triazolo[4,3
and triazolo[1,5
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Summary: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.
ISSN:1068-1620
1608-330X
DOI:10.1134/S1068162017040070