| Title : Synthesis and bioactivity of novel C2-glycosyl oxadiazole derivatives as acetylcholinesterase inhibitors - Wang_2018_Heterocycl.Commun_24_333 |
| Author(s) : Wang L , Wu YR , Ren ST , Yin L , Liu XJ , Cheng FC , Liu WW , Shi DH , Cao ZL , Sun HM |
| Ref : Heterocycl Commun , 24 :333 , 2018 |
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Abstract :
A series of glycosyl-substituted 1,3,4-oxadiazoles were synthesized by cyclization of glycosyl-acylthiosemicarbazides via a base-catalyzed reaction. The starting glycosyl-acylthiosemicarbazide derivatives were obtained by the reaction of glycosyl isothiocyanate with various hydrazides. The acetylcholinesterase (AChE) inhibitory activities of the products were tested by Ellman's method. The most active compounds were subsequently evaluated for the 50% inhibitory concentration (IC50) values. N-(1,-3,4,6-tetra-O-benzyl-2-deoxy-beta-D-glucopyranosyl)-5-(4-fluorophenyl)-1,3,4-oxadiazole-2-amine (6i) possesses the best AChE -inhibition activity with an IC50 of 1.61 +/- 0.34 microm. |
| PubMedSearch : Wang_2018_Heterocycl.Commun_24_333 |
| PubMedID: |
| Inhibitor | Tetrabenzyl-D-glucosamine-oxadiazole-6i |
Wang L, Wu YR, Ren ST, Yin L, Liu XJ, Cheng FC, Liu WW, Shi DH, Cao ZL, Sun HM (2018)
Synthesis and bioactivity of novel C2-glycosyl oxadiazole derivatives as acetylcholinesterase inhibitors
Heterocycl Commun
24 :333
Wang L, Wu YR, Ren ST, Yin L, Liu XJ, Cheng FC, Liu WW, Shi DH, Cao ZL, Sun HM (2018)
Heterocycl Commun
24 :333