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

Xiao Jian Xue, Yu Bin Wang, Peng Lu, Hai Feng Shang, Jin Xiong She, Ling Xian Xia, Hai Qian, Wen Long Huang

Research output: Contribution to journalArticle

5 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)524-527
Number of pages4
JournalChemical and Pharmaceutical Bulletin
Volume62
Issue number6
DOIs
StatePublished - Jun 2014
Externally publishedYes

Keywords

  • 1,3,4-thiadiazole
  • Acetylcholinesterase (AChE) inhibitor
  • Hybridization
  • Urea group

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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