[2,4-吡喃并[4',3':4,5]吡啶并[2,3-b]噻吩并[3,2-d]嘧啶的合成及其神经活性]

[Synthesis and Neurotropic Activity of 2,4-pyrano[4',3':4,5]pyrido[2,3-b]thieno[3,2-d] Pyrimidines].

作者信息

Paronikyan E G, Dashyan Sh Sh, Noravyan A S, Dzhagatspanyan I A, Paronikyan R G, Nazaryan I M, Akopyan A G

出版信息

Bioorg Khim. 2015 Nov-Dec;41(6):737-43. doi: 10.1134/s1068162015060126.

DOI:10.1134/s1068162015060126

Abstract

2,4-Disubstituted derivatives of pyrano[4',3':4,5]pyrido[2,3-b]thieno[3,2-d] pyrimidines were synthesized and their pharmacological studies was carried out at animals by the tests of antagonism with subcutaneous administration of corazol and behavior of "open field" model. The method of "rotating rod" was used to evaluate of neurotoxicity. The neurotropic properties were found in the new synthesized compounds. The new synthesized compounds as well as diazepam prevented the occurrence of clonic twitchings and clonic corazol seizures in animals. However, the studied compounds in contrast of tranquilizer diazepam having the anxiolytic and activating effects in the test of "open field", induced a oppressive behavior sedative effects.

摘要

合成了吡喃并[4',3':4,5]吡啶并[2,3 - b]噻吩并[3,2 - d]嘧啶的2,4 - 二取代衍生物，并通过皮下注射可拉佐的拮抗试验和“旷场”模型行为在动物身上进行了药理研究。采用“转棒”法评估神经毒性。在新合成的化合物中发现了亲神经特性。新合成的化合物以及地西泮可预防动物阵挛性抽搐和可拉佐阵挛性惊厥的发生。然而，与在“旷场”试验中具有抗焦虑和激活作用的镇静剂地西泮相比，所研究的化合物诱导出压抑行为的镇静作用。