92501-46-7

Upstream product

• 96077-49-5 1-carbethoxymethylene-6-methoxy-1,2,3,4-tetrahydroisoquinoline 
• 105-53-3 diethyl malonate 
• 36239-09-5 ethyl chlorocarbonylacetate 
• 2039-67-0 2-(3-methoxyphenyl)-1-ethanamine 
• 106840-17-9 N-(3-methoxy-phenethyl)-malonamic acid ethyl ester 

Downstream Products

• 649722-04-3 (6-hydroxy-1,2,3,4-tetrahydro-isoquinolin-1-yl)-acetic acid ethyl ester 
• 649722-11-2 dimethylcarbamic acid 1-[2-(4-nitrophenoxy)ethyl]-1,2,3,4-tetrahydroisoquinolin-6-yl ester 
• 649722-13-4 dimethylcarbamic acid 1-[2-(4-chlorophenoxy)ethyl]-1,2,3,4-tetrahydroisoquinolin-6-yl ester 

Relevant academic research and scientific papers

Compound and its as L-type calcium channel blocker or/and application of acetylcholine esterase inhibitors

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 conformational restriction approach to the development of dual inhibitors of acetylcholinesterase and serotonin transporter as potential agents for Alzheimer's disease

Alzheimer's disease (AD) has been treated with acetylcholinesterase (AChE) inhibitors such as donepezil. However, the clinical usefulness of AChE inhibitors is limited mainly due to their adverse peripheral effects. Depression seen in AD patients has been treated with serotonin transporter (SERT) inhibitors. We considered that combining SERT and AChE inhibition could improve the clinical usefulness of AChE inhibitors. In a previous paper, we found a potential dual inhibitor, 1, of AChE (IC50=101 nM) and SERT (IC50=42 nM), but its AChE inhibition activity was less than donepezil (IC50=10 nM). Here, we report the conformationally restricted (R)-18a considerably enhanced inhibitory activity against AChE (IC50=14 nM) and SERT (IC50=6 nM).

BENZYLAMINE ANALOGUE

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.