Structure-activity relationship, in vitro and in vivo evaluation of novel dienyl sulphonyl fluorides as selective BuChE inhibitors for the treatment of Alzheimer's disease

• Hoofdauteurs: Chengyao Wu (Auteur), Guijuan Zhang (Auteur), Zai-Wei Zhang (Auteur), Xia Jiang (Auteur), Ziwen Zhang (Auteur), Huanhuan Li (Auteur), Hua-Li Qin (Auteur), Wenjian Tang (Auteur)
• Formaat: Boek
• Gepubliceerd in: Taylor & Francis Group, 2021-01-01T00:00:00Z.
• Onderwerpen: article
• Online toegang: Connect to this object online.

To discover novel scaffolds as leads against dementia, a series of δ-aryl-1,3-dienesulfonyl fluorides with α-halo, α-aryl and α-alkynyl were assayed for ChE inhibitory activity, in which compound A10 was identified as a selective BuChE inhibitor (IC50 = 0.021 μM for eqBChE, 3.62 μM for hBuChE). SAR...