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新型乙酰胆碱酯酶抑制剂1,3,4-噻二唑-2-基脲衍生物的合成与体外评价

Synthesis and in vitro evaluation of 1,3,4-thiadiazol-2-yl urea derivatives as novel AChE inhibitors.

作者信息

Xue Xiao-jian, Wang Yu-bin, Lu Peng, Shang Hai-feng, She Jin-xiong, Xia Ling-xian, Qian Hai, Huang Wen-long

机构信息

School of Pharmaceutical Sciences, Nanjing University of Technology.

出版信息

Chem Pharm Bull (Tokyo). 2014;62(6):524-7. doi: 10.1248/cpb.c13-00964. Epub 2014 Apr 3.

Abstract

1,3,4-Thiadiazole and urea group were hybridized to form new molecular skeleton and 11 compounds were synthesized and evaluated as acetylcholinesterase (AChE) inhibitors. Most of them showed comparable effects in inhibition of AChE, especially compound 6b which exhibited activity with IC50 value 1.17 µM, as strong as galanthamine. This information offered by our research would be valuable for further investigation of structure-activity relationship (SAR) and useful in future research of AChE inhibitors.

摘要

将1,3,4-噻二唑和脲基团杂化以形成新的分子骨架,合成了11种化合物并将其作为乙酰胆碱酯酶(AChE)抑制剂进行评估。它们中的大多数在抑制AChE方面表现出相当的效果,尤其是化合物6b,其IC50值为1.17 μM,活性与加兰他敏一样强。我们的研究提供的这些信息对于进一步研究构效关系(SAR)将是有价值的,并且在未来AChE抑制剂的研究中有用。

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