Fluorosulfate-containing pyrazole heterocycles as selective BuChE inhibitors: structure-activity relationship and biological evaluation for the treatment of Alzheimer's disease

• Egile Nagusiak: Huan-Huan Li (Egilea), Chengyao Wu (Egilea), Shi-Long Zhang (Egilea), Jian-Guo Yang (Egilea), Hua-Li Qin (Egilea), Wenjian Tang (Egilea)
• Formatua: Liburua
• Argitaratua: Taylor & Francis Group, 2022-12-01T00:00:00Z.
• Gaiak: article
• Sarrera elektronikoa: Connect to this object online.

Novel scaffolds are expected to treat Alzheimer's disease, pyrazole-5-fluorosulfates were found as selective BuChE inhibitors. Compounds K1-K26 were assayed for ChE inhibitory activity, amongst them, compound K3 showed potent BuChE and hBuChE inhibition (IC50 = 0.79 μM and 6.59 μM). SAR analysi...