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

作者：Jung Jae Chul; Min Dongguk; Lim Heena; Moon Sohyeon; Jung Mankil; Oh Seikwan^*

来源：Medicinal Chemistry Research, 2013, 22(10): 4615-4621.

DOI：10.1007/s00044-012-0415-1

• Trans-3,4,5-trimethoxycinnamamides
• Condensation reaction
• Coupling reaction
• Antineurotoxicity
• Free radical scavenging
• Antinarcotic activity

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.

• 出版日期2013-10