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Literature summary for 3.1.1.8 extracted from

  • Dillon, G.P.; Gaynor, J.M.; Khan, D.; Carolan, C.G.; Ryder, S.A.; Marquez, J.F.; Reidy, S.; Gilmer, J.F.
    Isosorbide-based cholinesterase inhibitors; replacement of 5-ester groups leading to increased stability (2010), Bioorg. Med. Chem., 18, 1045-1053.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(benzylaminocarbonyloxy)-5-(phenylcarbonyloxyimino-)-1,4 3,6-dianhydro-D-glucitol 9% inhibition at 0.1 mM Homo sapiens
2-(benzylaminocarbonyloxy)-5-deoxy, 5-dehydro-((ethyloxycarbonyl)ene-)-1,4 3,6-dianhydro-D-glucitol 4.9% inhibition at 0.1 mM Homo sapiens
2-(benzylaminocarbonyloxy)-5-deoxy-5-phenylcarbonylamino-1,4 3,6-dianhydro-D-glucitol 46% inhibition at 0.1 mM Homo sapiens
2-(benzylaminocarbonyloxy)-5-deoxy-L-xylohex-6-enitol 9.8% inhibition at 0.1 mM Homo sapiens
2-(benzylaminocarbonyloxy)-5-keto-1,4 3,6-dianhydro-D-glucitol 10% inhibition at 0.1 mM Homo sapiens
2-(benzylaminocarbonyloxy)-5-ketoxime-1,4 3,6-dianhydro-D-glucitol 83% inhibition at 0.1 mM Homo sapiens
2-(benzylaminocarbonyloxy)-5-O-(phenylpropyloxy)-1,4 3,6-dianhydro-D-glucitol 55% inhibition at 0.1 mM Homo sapiens
2-(benzylaminocarbonyloxy)-5-O-benzyl-1,4 3,6-dianhydro-D-glucitol 55% inhibition at 0.1 mM Homo sapiens
5-deoxy-5-azido-1,4 3,6-dianhydro-D-glucitol 5% inhibition at 0.1 mM Homo sapiens
7-exo-(benzylaminocarbonyloxy)-3-oxo-2,5,9-trioxabicyclo [4.3.0] nonane 10% inhibition at 0.1 mM Homo sapiens
isosorbide-di-(4-nitrophenyl carbamate)
-
Homo sapiens
isosorbide-di-(benzylcarbamate) 77% inhibition at 0.1 mM Homo sapiens
isosorbide-di-(butylcarbamate) 13% inhibition at 0.1 mM Homo sapiens
isosorbide-di-(ethylcarbamate)
-
Homo sapiens
isosorbide-di-(propylcarbamate) 28% inhibition at 0.1 mM Homo sapiens
isosorbide-di-phenylcarbamate 77% inhibition at 0.1 mM Homo sapiens
N-methyl-7-exo-(benzylaminocarbonyloxy-)-3-oxo-5,9-dioxa-2-azabicyclo[4.3.0] nonane 6.5% inhibition at 0.1 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
butyrylthiocholine + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
BChE
-
Homo sapiens
butyrylcholinesterase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0054
-
-
Homo sapiens isosorbide-di-(4-nitrophenyl carbamate)
0.0065
-
-
Homo sapiens isosorbide-di-(ethylcarbamate)