649722-87-2

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 649722-86-1 dimethyl-carbamic acid 1-[2-(4-nitro-phenoxy)-ethyl]-5-oxo-2,3,4,5-tetrahydro-1H-benzo[c]azepin-7-yl ester 
• 95-01-2 2,4-Dihydroxybenzaldehyde 
• 444646-64-4 4-formyl-3-hydroxy-phenyl dimethylcarbamate 
• 444646-66-6 dimethylcarbamic acid 4-formyl-3-vinylphenyl ester 
• 444646-68-8 4-(1,3-dihydroxy-propyl)-3-vinyl-phenyl dimethylcarbamate 
• 444646-65-5 5-dimethylcarbamoyloxy-2-formyl-phenyl trifluoromethanesulfonate 
• 444646-74-6 7-dimethylcarbamoyloxy-1-(2-hydroxyethyl)-1,3-dihydrobenzo[c]azepine-2-carboxylic acid tert-butyl ester 
• 649722-85-0 7-dimethylcarbamoyloxy-1-(2-hydroxyethyl)-5-oxo-1,3,4,5-tetrahydrobenzo[c]azepine-2-carboxylic acid tert-butyl ester 
• 444646-69-9 dimethylcarbamic acid 4-[3-(tert-butyldiphenylsilanyloxy)-1-hydroxypropyl]-3-vinylphenyl ester 
• 649722-52-1 4-[1-bromo-3-(t-butyl-diphenyl-silanyloxy)-1-hydroxy-propyl]-3-vinyl-phenyl dimethylcarbamate 
• 649722-53-2 4-[1-allylamino-3-(t-butyl-diphenyl-silanyloxy)-1-hydroxy-propyl]-3-vinyl-phenyl dimethylcarbamate 
• 444646-73-5 t-Butyl 1-[2-(t-butyl-diphenyl-silanyloxy)-ethyl]-7-dimethylcarbamoyloxy-1,3-dihydro-benzo[c]azepine-2-carboxylate 
• 444646-72-4 allyl[3-(tert-butyldiphenylsilanyloxy)-1-(4-dimethylcarbamoyloxy-2-vinylphenyl)propyl]carbamic acid tert-butyl ester 

Downstream Products

• 649722-88-3 7-dimethylcarbamoyloxy-5-methylene-1-[2-(4-nitro-phenoxy)-ethyl]-1,3,4,5-tetrahydro-benzo[c]azepine-2-carboxylic acid tert-butyl ester 
• 649722-91-8 7-dimethylcarbamoyloxy-1-[2-(4-nitrophenoxy)ethyl]-5-trifluoromethanesulfonyloxy-1,3-dihydrobenzo[c]azepine-2-carboxylic acid tert-butyl ester 
• 649723-07-9 dimethyl-carbamic acid 5-methyl-1-[2-(4-nitro-phenoxy)-ethyl]-2,3-dihydro-1H-benzo[c]azepin-7-yl ester 
• 649723-08-0 dimethyl-carbamic acid 1-[2-(4-nitro-phenoxy)-ethyl]-5-vinyl-2,3-dihydro-1H-benzo[c]azepin-7-yl ester 
• 649723-09-1 dimethyl-carbamic acid 1-[2-(4-nitro-phenoxy)-ethyl]-5-thiophen-2-yl-2,3-dihydro-1H-benzo[c]azepin-7-yl ester 
• 649722-92-9 7-dimethylcarbamoyloxy-5-methyl-1-[2-(4-nitro-phenoxy)-ethyl]-1,3-dihydro-benzo[c]azepine-2-carboxylic acid tert-butyl ester 
• 649723-02-4 dimethyl-carbamic acid 5-(4-chloro-phenyl)-1-[2-(4-nitro-phenoxy)-ethyl]-2,3-dihydro-1H-benzo[c]azepin-7-yl ester 
• 649722-95-2 7-dimethylcarbamoyloxy-1-[2-(4-nitro-phenoxy)-ethyl]-5-vinyl-1,3-dihydro-benzo[c]azepine-2-carboxylic acid tert-butyl ester 
• 649722-98-5 7-dimethylcarbamoyloxy-1-[2-(4-nitro-phenoxy)-ethyl]-5-thiophen-2-yl-1,3-dihydro-benzo[c]azepine-2-carboxylic acid tert-butyl ester 
• 649723-01-3 5-(4-chloro-phenyl)-7-dimethylcarbamoyloxy-1-[2-(4-nitro-phenoxy)-ethyl]-1,3-dihydro-benzo[c]azepine-2-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

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).