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

4 Citations (Scopus)

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 - Jan 1 2014

Fingerprint

Cholinesterase Inhibitors
Urea
Galantamine
Derivatives
Structure-Activity Relationship
Acetylcholinesterase
Skeleton
Inhibitory Concentration 50
Research
In Vitro Techniques
1,3,4-thiadiazole

Keywords

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

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

Cite this

Synthesis and in vitro evaluation of 1,3,4-thiadiazol-2-yl urea derivatives as novel AChE inhibitors. / Xue, Xiao Jian; Wang, Yu Bin; Lu, Peng; Shang, Hai Feng; She, Jin-Xiong; Xia, Ling Xian; Qian, Hai; Huang, Wen Long.

In: Chemical and Pharmaceutical Bulletin, Vol. 62, No. 6, 01.01.2014, p. 524-527.

Research output: Contribution to journalArticle

Xue, Xiao Jian ; Wang, Yu Bin ; Lu, Peng ; Shang, Hai Feng ; She, Jin-Xiong ; Xia, Ling Xian ; Qian, Hai ; Huang, Wen Long. / Synthesis and in vitro evaluation of 1,3,4-thiadiazol-2-yl urea derivatives as novel AChE inhibitors. In: Chemical and Pharmaceutical Bulletin. 2014 ; Vol. 62, No. 6. pp. 524-527.
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