Ligustrazine derivative as well as preparation method and medical application thereof

• Main Authors: FANG YUANYING, LEE HYE-RAN, ZENG QING, YANG ZUNHUA, CAI ZHIFANG, FENG YULIN, ZHANG ZIWEI, YING YUQI
• Format: Patent
• Language: Chinese; English
• Published: 27.10.2023
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention relates to a ligustrazine derivative and a preparation method and medical application thereof.The compound is prepared by taking substituted benzofuranone or substituted indanone as an initial raw material through a condensation reaction, and the obtained compound can remarkably improve the survival rate of cerebral cortex neuronal cells under the hypoxia and sugar deficiency condition; the cerebral infarction area and the neurological function of an ischemia/reperfusion rat model can be obviously improved. The synthesis method of the compound is simple, and raw materials are cheap and easy to obtain, so that the compound is suitable for industrial application. 本发明涉及一种川芎嗪衍生物、其制备方法及医药用途，本发明化合物以取代的苯并呋喃酮或取代茚酮为起始原料，经缩合反应制备，得到的化合物能够在缺氧缺糖的条件下显著提高大脑皮层神经元细胞的存活率，而且能够显著改善缺血/再灌注大鼠模型的脑梗死面积和神经功能。本发明化合物合成方法简单，原料廉价易得，因此适合产业化应用。