A simple synthesis of trans -3,4,5-trimethoxycinnamamides and evaluation of their biologic activity

Medicinal Chemistry Research(2013)

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摘要
A simple synthesis and biologic evaluation of trans -3,4,5-trimethoxycinnamamides 10a–e and 11 as novel antinarcotic agents is described. The synthetic key strategies involve condensation reaction and coupling reaction to generate trans -3,4,5-trimethoxycinnamamides 10a–e and 11 . They were evaluated for free radical scavenging, inhibitory action for neurotoxicity in cultured neurons, and antinarcotic activity in mice. It was found that compounds 10a , 10d , and 10e displayed significant inhibitory action of the glutamate-induced neurotoxicity and 10a–e and 11 showed high antinarcotic activity in mice.
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关键词
Trans-3,4,5-trimethoxycinnamamides, Condensation reaction, Coupling reaction, Antineurotoxicity, Free radical scavenging, Antinarcotic activity
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