摘要
以他克林为先导物 ,设计合成了 14个未见文献报道的新化合物 ,其中目的物 8个 .初步药理试验结果表明 ,所合成的目的物中 (3b)、(3f)和 (3h)活性较好 ,显示 9 位氨基、巯基和羧基取代物均有神经细胞保护作用 .由于化合物 (3f)为他克林的苯并类似物 。
Alzheimer′s dementia(AD)is a neurodegenerative disease.It was assumed to achieve proper balance of the modulatory effects on diverse neurotransmitter systems in a single molecule for the treatment of AD.On the basis of tacrine as the lead compound,eight new derivatives of tetrahydroacridine were designed and synthesized.The preliminary bioactivity study showed that compounds(3b),(3f),(3h)had better protective effects on glutamic acid induced nerve cell trauma than tacrine.
出处
《中国药物化学杂志》
CAS
CSCD
2000年第3期172-175,共4页
Chinese Journal of Medicinal Chemistry
基金
江苏省自然科学基金!No .BK970 80
关键词
四氢吖啶
他克林
神经细胞保护
合成
tetrahydroacridine
tacrine
nerve cell protection
synthesis
