含氨基酸小分子N型钙通道阻滞剂的合成及其镇痛活性Synthesis and analgesic activity of novel L-amino acid based small molecule N-type calcium channel blockers
王倩倩,李娜,尹延彦,白素平
WANG Qian-qian1,LI Na2,YIN Yan-yan1,BAI Su-ping1(1.College of Pharmacy
摘要(Abstract):
目的获得具有镇痛活性的小分子化合物。方法设计合成了8个含氨基酸的小分子化合物,并用小鼠热板法进行镇痛活性的测定。结果用简便的方法合成了8个目标化合物,药理结果表明,部分化合物具有一定的生物活性。结论化合物5d、5f效果较好,可以作为先导化合物进行研究。
Objective To obtain small molecule compounds possessing analgesic activity.Methods Eight L-amino acid based small molecules were designed and synthesized and their analgesic activities were evaluated by the rat hot pat pain model.Results Synthesized target compounds by convenient method and the result of pharmacology indicated part of these compounds possessed analgesic activity.Conclusions The results show that compound 5d and 5f possess the better analgesic activity which can be a lead compound for the further modification.
关键词(KeyWords):
N型钙通道阻滞剂;含氨基酸的小分子;镇痛活性;合成
N-type calcium channel blocker;L-amino acid based small molecule compound;analgesic activity;synthesis
基金项目(Foundation): 国家自然科学基金资助项目(81072552)
作者(Author):
王倩倩,李娜,尹延彦,白素平
WANG Qian-qian1,LI Na2,YIN Yan-yan1,BAI Su-ping1(1.College of Pharmacy
DOI: 10.14066/j.cnki.cn21-1349/r.2012.06.010
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- N型钙通道阻滞剂
- 含氨基酸的小分子
- 镇痛活性
- 合成
N-type calcium channel blocker - L-amino acid based small molecule compound
- analgesic activity
- synthesis