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Literature summary for 3.1.1.7 extracted from

  • Madaiah, M.; Jayanna, B.K.; Manu, A.S.; Prashanth, M.K.; Revanasiddappa, H.D.; Veeresh, B.
    Synthesis, characterization, and evaluation of difluoropyrido[4,3-b]indoles as potential agents for acetylcholinesterase and antiamnesic activity (2017), Arch. Pharm., 350, e1600303 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4,4-difluoro-8-(propan-2-yl)-N-(2,3,4-trifluorophenyl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
4,4-difluoro-8-(propan-2-yl)-N-propyl-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
4,4-difluoro-N,8-di(propan-2-yl)-1,3,4,5-tetrahydro-2Hpyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
4,4-difluoro-N-(2-fluorophenyl)-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
4,4-difluoro-N-(3-fluorophenyl)-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
4,4-difluoro-N-(4-fluorophenyl)-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
donepezil
-
Rattus norvegicus
additional information synthesis of difluoropyrido[4,3-b]indoles and evaluation as acetylcholinesterase inhibitors, anti-amnesic effect of synthesized compounds against scopolamine-induced memory loss, overview Rattus norvegicus
N-(2,4-difluorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(2,4-dimethylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(2,5-difluorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(2,6-difluorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(2-chlorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(2-cyanophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(2-methoxyphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(2-methylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(3,4-difluorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(3,4-dimethylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(3,5-dimethylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(3-chlorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(3-ethylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(3-methylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(4-methoxyphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-(4-methylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-cyclopentyl-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
N-ethyl-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
-
Rattus norvegicus
neostigmine
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
acetylcholine + H2O Rattus norvegicus
-
choline + acetate
-
?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylcholine + H2O
-
Rattus norvegicus choline + acetate
-
?
acetylthiocholine + H2O
-
Rattus norvegicus thiocholine + acetate
-
?

Synonyms

Synonyms Comment Organism
AChE
-
Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000067
-
pH 7.4, temperature not specified in the publication Rattus norvegicus donepezil
0.0000462
-
pH 7.4, temperature not specified in the publication Rattus norvegicus neostigmine
0.0000476
-
pH 7.4, temperature not specified in the publication Rattus norvegicus 4,4-difluoro-8-(propan-2-yl)-N-(2,3,4-trifluorophenyl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000483
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(2,6-difluorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000494
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(2,5-difluorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000499
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-difluorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000508
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(2,4-difluorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000515
-
pH 7.4, temperature not specified in the publication Rattus norvegicus 4,4-difluoro-N-(4-fluorophenyl)-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000527
-
pH 7.4, temperature not specified in the publication Rattus norvegicus 4,4-difluoro-N-(3-fluorophenyl)-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000563
-
pH 7.4, temperature not specified in the publication Rattus norvegicus 4,4-difluoro-N-(2-fluorophenyl)-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000653
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(2-cyanophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000967
-
pH 7.4, temperature not specified in the publication Rattus norvegicus 4,4-difluoro-8-(propan-2-yl)-N-propyl-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000987
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(2-methoxyphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0000991
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-cyclopentyl-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001014
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-ethyl-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001023
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(4-methylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001024
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3-ethylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001039
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(2-methylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001039
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(4-methoxyphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001052
-
pH 7.4, temperature not specified in the publication Rattus norvegicus 4,4-difluoro-N,8-di(propan-2-yl)-1,3,4,5-tetrahydro-2Hpyrido[4,3-b]indole-2-carboxamide
0.0001156
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3-methylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001682
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3-chlorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001684
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,5-dimethylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001686
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(2,4-dimethylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001739
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(2-chlorophenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide
0.0001739
-
pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-dimethylphenyl)-4,4-difluoro-8-(propan-2-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide