2689-47-6Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase
Liu, Siyu,Pistolozzi, Marco,Tan, Wen,Wu, Jie
, (2020/02/05)
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.
Compound as well as preparation method and application thereof
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Paragraph 0062; 0063; 0064, (2019/01/06)
The invention discloses a compound as well as a preparation method and application thereof and belongs to the field of medicines. The compound is a carbamyl ester derivative of a phenylethanolamine structure, and has a chemical structure formula (I) shown in the specification. The compound has remarkable functions of inhibiting acetylcholin esterase and butyrylcholine esterase, can be used as a double-target cholinesterase inhibitor, and can be also applied to preparation of medicines for treating diseases related to cholinesterase.
Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors
Wang, Ling,Wang, Yu,Tian, Yiguang,Shang, Jinling,Sun, Xiaoou,Chen, Hongzhuan,Wang, Hao,Tan, Wen
, p. 360 - 371 (2016/12/22)
A series of novel chalcone-rivastigmine hybrids were designed, synthesized, and tested in vitro for their ability to inhibit human acetylcholinesterase and butyrylcholinesterase. Most of the target compounds showed hBChE selective activity in the micro- a
Compound and its as L-type calcium channel blocker or/and application of acetylcholine esterase inhibitors
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Paragraph 0223; 0224, (2016/10/07)
Disclosed in this invention are compounds and the uses as L-type calcium channel blocker and/or acetylcholinesterase inhibitor thereof. The uses of said compounds in the manufactures of a medicament for the treatment of cardiovascular diseases, apoplexy or senile dementia are also disclosed in the present invention.
A kind of carbamate-koncar ketone choline esterase inhibitor and its preparation method and application (by machine translation)
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Paragraph 0148; 0149; 0160, (2016/11/28)
The present invention discloses a kind of carbamate-koncar ketone choline esterase inhibitor and its preparation method and application, belongs to the field of medicinal chemistry. Cholinesterase inhibitors of the invention represented by general formula
Rhodium-catalyzed selective C-H activation/olefination of phenol carbamates
Gong, Tian-Jun,Xiao, Bin,Liu, Zhao-Jing,Wan, Jian,Xu, Jun,Luo, Dong-Fen,Fu, Yao,Liu, Lei
supporting information; experimental part, p. 3235 - 3237 (2011/08/22)
Rh(III)-catalyzed ortho C-H activation/olefination of phenol carbamates has been developed. High regioselectivity is observed with a range of phenol carbamates enabling efficient coupling with acrylates and styrenes. This reaction exhibits different react
BENZYLAMINE ANALOGUE
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Page/Page column 69, (2008/06/13)
A compound of the formula (I): [wherein R1 represents a C1-C6 alkyl group etc., R2 and R3 are the same or different and represent a hydrogen atom etc., Ra represents a C1-C6 alkyl group etc., Arom represents an aryl group etc., A represents a C1-C6 alkylene group, E represents a single bond, an oxygen atom, a sulfur atom etc., X1 and X2 are the same or different and represent an oxygen atom or a sulfur atom] or a pharmacologically acceptable salt or ester thereof.
