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吡啶并吡嗪酮和吡啶并二氮杂䓬酮衍生物的合成及其对中枢神经系统的活性

Synthesis and CNS activities of pyridopyrazinone and pyridodiazepinone derivatives.

作者信息

Savelli F, Boido A, Satta M, Peana A, Marzano C

机构信息

Istituto di Scienze Farmaceutiche, Università di Genova, Italy.

出版信息

Farmaco. 1994 Apr;49(4):259-65.

PMID:8049005
Abstract

New tricyclic derivatives with cyclocondensed pyrido-pyrazine 7,10 and pyrido-diazepine 20a,20b skeletons were synthetized and biologically investigated. The compounds, preliminarily tested on explorative, muscle relaxing, antinociceptive, spontaneous motor activities and influence on the narcotic effect of Evipan, revealed interesting CNS depressant and analgesic activities. The pyrido[2,3-e]pyrrolo[1,2-a]pyrazine structure of 7 appeared the most promising for analgesic and neuroleptic activities. The above compounds were assayed also for their capacity to inhibit DNA synthesis in Ehrlich ascites tumor cells; 20a appeared to be able of inducing a significant inhibition.

摘要

合成了具有稠合吡啶并吡嗪7,10和吡啶并二氮杂卓20a,20b骨架的新型三环衍生物,并进行了生物学研究。对这些化合物进行了探索性、肌肉松弛、抗伤害感受、自发运动活性以及对依托咪酯麻醉作用影响的初步测试,结果显示出有趣的中枢神经系统抑制和镇痛活性。7的吡啶并[2,3 - e]吡咯并[1,2 - a]吡嗪结构在镇痛和抗精神病活性方面似乎最有前景。还测定了上述化合物抑制艾氏腹水瘤细胞DNA合成的能力;20a似乎能够诱导显著的抑制作用。

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