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Literature summary for 3.1.3.11 extracted from

  • Dang, Q.; Kasibhatla, S.R.; Jiang, T.; Fan, K.; Liu, Y.; Taplin, F.; Schulz, W.; Cashion, D.K.; Reddy, K.R.; van Poelje, P.D.; Fujitaki, J.M.; Potter, S.C.; Erion, M.D.
    Discovery of phosphonic diamide prodrugs and their use for the oral delivery of a series of fructose 1,6-bisphosphatase inhibitors (2008), J. Med. Chem., 51, 4331-4339.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-amino-4-[2-(5-N,N'-bis((S)-1-(1-ethoxycarbonyl)ethyl)phosphonoamido)furanyl]-5-isobutylthiazole optimization of the diamide prodrugs of phosphonic acid leads to the identification of a new diamide, the first reported orally efficacious FBPase inhibitor Homo sapiens
2-amino-4-[2-(5-phosphono)furanyl]-5-ethoxycarbonylthiazole potent FBPase inhibitor Homo sapiens
2-amino-4-[2-(5-phosphono)furanyl]-5-ethoxycarbonylthiazole potent FBPase inhibitor: when administerd intravenously it lowers plasma glucose levels in 18 h fasted normal Sprague-Dawley rats above 50% at doses below 10 mg/kg Rattus norvegicus
2-amino-4-[2-(5-phosphono)furanyl]-5-isobutylthiazole potent FBPase inhibitor Homo sapiens
2-amino-4-[2-(5-phosphono)furanyl]-5-isobutylthiazole potent FBPase inhibitor: when administerd intravenously it lowers plasma glucose levels in 18 h fasted normal Sprague-Dawley rats above 50% at doses below 10 mg/kg Rattus norvegicus
2-amino-4-[2-(5-phosphono)furanyl]-5-phenylthiazole potent FBPase inhibitor Homo sapiens
2-amino-4-[2-(5-phosphono)furanyl]-5-phenylthiazole potent FBPase inhibitor: when administerd intravenously it lowers plasma glucose levels in 18 h fasted normal Sprague-Dawley rats above 50% at doses below 10 mg/kg Rattus norvegicus
2-amino-4-[2-(5-phosphono)furanyl]-5-propylsulfanylthiazole potent FBPase inhibitor Homo sapiens
2-amino-4-[2-(5-phosphono)furanyl]-5-propylsulfanylthiazole potent FBPase inhibitor: when administerd intravenously it lowers plasma glucose levels in 18 h fasted normal Sprague-Dawley rats above 50% at doses below 10 mg/kg Rattus norvegicus
2-amino-5-methylsulfanyl-4-[2-(5-diethylphosphono)furanyl]thiazole potent FBPase inhibitor Homo sapiens
2-amino-5-methylsulfanyl-4-[2-(5-diethylphosphono)furanyl]thiazole potent FBPase inhibitor: when administerd intravenously it lowers plasma glucose levels in 18 h fasted normal Sprague-Dawley rats above 50% at doses below 10 mg/kg Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
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Rattus norvegicus
-
-
-

Synonyms

Synonyms Comment Organism
FBPase
-
Homo sapiens
FBPase
-
Rattus norvegicus
fructose 1,6-bisphosphatase
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Homo sapiens
fructose 1,6-bisphosphatase
-
Rattus norvegicus