Synthesis and in vitro evaluation of 1,3,4-thiadiazol-2-yl urea derivatives as novel AChE inhibitors.
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.
School of Pharmaceutical Sciences, Nanjing University of Technology.
Xiao-jian
XJ
Xue
Yu-bin
YB
Wang
Peng
P
Lu
Hai-feng
HF
Shang
Jin-xiong
JX
She
Ling-xian
LX
Xia
Hai
H
Qian
Wen-long
WL
Huang
D000110:Acetylcholinesterase / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
C000595928:1-(5-(4-methoxyphenyl)-1,3,4-thiadiazol-2-yl)-3-(pyridine-3-yl)urea; D002800:Cholinesterase Inhibitors; D013830:Thiadiazoles; D014508:Urea; D000110:Acetylcholinesterase