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(1R,2R,6S)-3-甲基-6-(1-丙烯-2-基)环己-3-烯-1,2-二醇在帕金森病动物模型中的高活性。

Highly potent activity of (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol in animal models of Parkinson's disease.

机构信息

Russian Academy of Sciences, Novosibirsk, Russian Federation.

出版信息

J Med Chem. 2011 Jun 9;54(11):3866-74. doi: 10.1021/jm2001579. Epub 2011 May 13.

Abstract

(1R,2R,6S)-3-Methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol 1 possesses potent antiparkinsonian activity in both MPTP and haloperidol animal models. The use of compound 1 resulted in nearly full recovery of the locomotor and exploratory activities and was as effective as the comparator agent (levodopa). All eight stereoisomers of compound 1 have been synthesized and the influence of the absolute configuration on the antiparkinsonian activity of compound 1 was shown.

摘要

(1R,2R,6S)-3-甲基-6-(1-丙烯基)环己-3-烯-1,2-二醇 1 在 MPTP 和氟哌啶醇动物模型中均具有很强的抗帕金森病活性。使用化合物 1 可使运动和探索活动几乎完全恢复,其效果与对照剂(左旋多巴)相当。1 的 8 个立体异构体均已合成,并表明了绝对构型对 1 的抗帕金森病活性的影响。

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