Category: indole-building-block. In 2020.0 BIOORGAN MED CHEM published article about ALZHEIMERS-DISEASE; STEREOSELECTIVE INHIBITION; BAMBUTEROL; CHOLINESTERASES; DEMENTIA; KINETICS; UPDATE in [Wu, Jie] Jinan Univ, Sch Pharm, Guangzhou 510632, Peoples R China; [Wu, Jie] YZ Hlth Tech Inc, Zhuhai 519000, Peoples R China; [Pistolozzi, Marco] South China Univ Technol, Sch Biol & Biol Engn, Guangzhou 510006, Peoples R China; [Liu, Siyu; Tan, Wen] Guangdong Univ Technol, Inst Biomed & Pharmaceut Sci, Guangzhou 510006, Peoples R China; [Tan, Wen] Monash Univ Malaysia, Jeffrey Cheah Sch Med & Hlth Sci, Bandar Sunway 47500, Selangor Darul, Malaysia in 2020.0, Cited 33.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.
Rivastigmine, a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), has been approved by U.S. Food and Drug Administration to treat Alzheimer’s disease (AD) and Parkinson’s disease (PD) dementia. In the current work, a bambuterol derivative lacking one of the carbamoyloxy groups on the benzene ring (BMC-1) and its analogues were synthesized using 1-(3-hydroxyphenyl) ethan-1-one and 1-(4-hydroxyphenyl) ethan-1-one as starting materials. In-vitro cholinesterase assay established that nine compounds were more potent to inhibit both electric eel AChE and equine serum BChE than rivastigmine under the same experimental conditions. Further study confirmed that among the nine carbamates, BMC-3 (IC50(AChE) = 792 nM, IC50(BChE) = 2.2 nM) and BMC-16 (IC50(AChE) = 266 nM, IC50(BChE) = 10.6 nM) were excellent cholinesterase inhibitors with potential of permeating through the blood-brain barrier. These carbamates could be used as potential dual inhibitors of AChE and BChE and to discover novel drugs for the treatment of AD and PD dementia.
Category: indole-building-block. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Wu, J; Pistolozzi, M; Liu, SY; Tan, W or concate me.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles