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

doi:10.1248/cpb.c13-00964

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 journal › Article › peer-review

9 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 language	English (US)
Pages (from-to)	524-527
Number of pages	4
Journal	Chemical and Pharmaceutical Bulletin
Volume	62
Issue number	6
DOIs	https://doi.org/10.1248/cpb.c13-00964
State	Published - Jun 2014
Externally published	Yes

Keywords

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

ASJC Scopus subject areas

Chemistry(all)
Drug Discovery

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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.",

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AU - Xue, Xiao Jian

AU - Wang, Yu Bin

AU - Lu, Peng

AU - Shang, Hai Feng

AU - She, Jin Xiong

AU - Xia, Ling Xian

AU - Qian, Hai

AU - Huang, Wen Long

PY - 2014/6

Y1 - 2014/6

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AB - 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.

KW - 1,3,4-thiadiazole

KW - Acetylcholinesterase (AChE) inhibitor

KW - Hybridization

KW - Urea group

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

Abstract

Keywords

ASJC Scopus subject areas

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