Heterocycles p. 275 - 286 (2015)
Update date:2022-08-16
Topics:
Liu, Wei-Wei
Li, Qu-Xiang
Shi, Da-Hua
Cao, Zhi-Ling
Cheng, Feng-Chang
Tao, Chuan-Zhou
Yin, Long
Wang, Xuan
The corresponding 4-substituted glycosyl thiosemicarbazide derivatives (6a-6l) were obtained by the reaction of glycosyl isothiocyanate 4 with various hydrazides. Further cyclization with the system of p-TsCl/TEA led to the formation of N-glycosyl-5-substituted 1,3,4-thiadiazole-2-amine (7a-7l). Subsequent removal of the acetyl groups were conducted using the system of NaOMe/MeOH. The chemical structures of all new products were confirmed by IR, 1H NMR and ESI-HRMS. The acetylcholinesterase (AChE) inhibitory activities of those compounds were tested by Ellman's method. Among them, the compound 8h possessed the best acetylcholinesterase-inhibition activity with IC50 of 18.38 ± 0.89 μM.
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