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Literature summary for 3.1.1.7 extracted from

  • Bohn, P.; Le Fur, N.; Hagues, G.; Costentin, J.; Torquet, N.; Papamicael, C.; Marsais, F.; Levacher, V.
    Rational design of central selective acetylcholinesterase inhibitors by means of a bio-oxidisable prodrug strategy (2009), Org. Biomol. Chem., 7, 2612-2618.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-methyl-3-(methylcarbamoyl)-1,4-dihydroquinolin-5-yl dimethylcarbamate
-
Homo sapiens
1-methyl-3-(morpholin-4-ylcarbonyl)-1,4-dihydroquinolin-5-yl dimethylcarbamate
-
Homo sapiens
3-(dimethylcarbamoyl)-1-methyl-1,4-dihydroquinolin-5-yl dimethylcarbamate
-
Homo sapiens
3-(dimethylcarbamoyl)-5-[(dimethylcarbamoyl)oxy]-1-methylquinolinium
-
Homo sapiens
5-[(dimethylcarbamoyl)oxy]-1-methyl-3-(methylcarbamoyl)quinolinium
-
Homo sapiens
5-[(dimethylcarbamoyl)oxy]-1-methyl-3-(morpholin-4-ylcarbonyl)quinolinium
-
Homo sapiens
5-[(dimethylcarbamoyl)oxy]-3-(ethoxycarbonyl)-1-methylquinolinium
-
Homo sapiens
5-[(dimethylcarbamoyl)oxy]-3-(methoxycarbonyl)-1-methylquinolinium
-
Homo sapiens
5-[(ethylcarbamoyl)oxy]-3-(methoxycarbonyl)-1-methylquinolinium
-
Homo sapiens
7-[(dimethylcarbamoyl)oxy]-3-(ethoxycarbonyl)-1-methylquinolinium
-
Homo sapiens
donepezil
-
Homo sapiens
ethyl 5-[(dimethylcarbamoyl)oxy]-1-methyl-1,4-dihydroquinoline-3-carboxylate
-
Homo sapiens
ethyl 7-[(dimethylcarbamoyl)oxy]-1-methyl-1,4-dihydroquinoline-3-carboxylate
-
Homo sapiens
galanthamine
-
Homo sapiens
methyl 5-[(dimethylcarbamoyl)oxy]-1-methyl-1,4-dihydroquinoline-3-carboxylate
-
Homo sapiens
methyl 5-[(ethylcarbamoyl)oxy]-1-methyl-1,4-dihydroquinoline-3-carboxylate
-
Homo sapiens
additional information synthesis of a set of 1,4-dihydroquinolines and their corresponding quinolinium salts as potential enzyme inhibitors, overview. All reduced forms are unable to exhibit any anticholinesterase activity, while most of the quinolinium salts display high AChE inhibitory activity with IC50 values ranging from 0.006 mM to 7 nM. Design of a bio-oxidisable prodrug for central selective AChE inhibitory activity Homo sapiens
rivastigmine
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
AChE
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000007
-
-
Homo sapiens 5-[(dimethylcarbamoyl)oxy]-3-(ethoxycarbonyl)-1-methylquinolinium
0.000015
-
-
Homo sapiens 3-(dimethylcarbamoyl)-5-[(dimethylcarbamoyl)oxy]-1-methylquinolinium
0.000029
-
-
Homo sapiens 5-[(dimethylcarbamoyl)oxy]-1-methyl-3-(methylcarbamoyl)quinolinium
0.00005
-
-
Homo sapiens donepezil
0.00011
-
-
Homo sapiens 5-[(dimethylcarbamoyl)oxy]-3-(methoxycarbonyl)-1-methylquinolinium
0.0005
-
-
Homo sapiens 7-[(dimethylcarbamoyl)oxy]-3-(ethoxycarbonyl)-1-methylquinolinium
0.00086
-
-
Homo sapiens 5-[(dimethylcarbamoyl)oxy]-1-methyl-3-(morpholin-4-ylcarbonyl)quinolinium
0.006
-
-
Homo sapiens 5-[(ethylcarbamoyl)oxy]-3-(methoxycarbonyl)-1-methylquinolinium
1
-
above Homo sapiens methyl 5-[(dimethylcarbamoyl)oxy]-1-methyl-1,4-dihydroquinoline-3-carboxylate
1
-
above Homo sapiens methyl 5-[(ethylcarbamoyl)oxy]-1-methyl-1,4-dihydroquinoline-3-carboxylate
1
-
above Homo sapiens ethyl 5-[(dimethylcarbamoyl)oxy]-1-methyl-1,4-dihydroquinoline-3-carboxylate
1
-
above Homo sapiens ethyl 7-[(dimethylcarbamoyl)oxy]-1-methyl-1,4-dihydroquinoline-3-carboxylate
1
-
above Homo sapiens 1-methyl-3-(morpholin-4-ylcarbonyl)-1,4-dihydroquinolin-5-yl dimethylcarbamate
1
-
above Homo sapiens 3-(dimethylcarbamoyl)-1-methyl-1,4-dihydroquinolin-5-yl dimethylcarbamate
1
-
above Homo sapiens 1-methyl-3-(methylcarbamoyl)-1,4-dihydroquinolin-5-yl dimethylcarbamate