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3-(4,4-二甲基-2-哌啶酮-6-基)甲基-2-吡唑啉衍生物的合成

Synthesis of 3-(4,4-dimethyl-2-piperidon-6-yl)methyl-2-pyrazoline derivatives.

作者信息

Sedzik-Hibner D, Czuba W, Lewandowska A

出版信息

Pol J Pharmacol Pharm. 1985 Sep-Oct;37(5):685-92.

PMID:3879537
Abstract

The results of studies of condensation of 1-(4,4-dimethyl-2-piperidon-6-yl)-4-phenyl-3-buten-2-one and its derivatives substituted in the benzene ring (R = 4-CH3 and R = 4-Cl) with hydrazine and its methyl or phenyl derivative are described. Compounds 2a, 2c and 2g were tested for their possible action on the central nervous system. Two drugs: 2c and 2g decreased locomotor activity. None of the examined compounds inhibited the reserpine-induced hypothermia, 5-HT syndrome and convulsions induced by pentetrazole in mice. Compound 2c injected only intraperitoneally depressed the number of the writhing episodes induced by p-phenylbenzoquinone.

摘要

描述了1-(4,4-二甲基-2-哌啶酮-6-基)-4-苯基-3-丁烯-2-酮及其在苯环上被取代的衍生物(R = 4-CH₃和R = 4-Cl)与肼及其甲基或苯基衍生物缩合反应的研究结果。对化合物2a、2c和2g进行了对中枢神经系统可能作用的测试。两种药物:2c和2g降低了运动活性。所检测的化合物均未抑制小鼠中利血平诱导的体温过低、5-羟色胺综合征和戊四氮诱导的惊厥。仅腹腔注射的化合物2c可抑制对苯醌诱导的扭体发作次数。

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