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Literature summary for 1.2.1.104 extracted from

  • He, J.B.; He, H.F.; Zhao, L.L.; Zhang, L.; You, G.Y.; Feng, L.L.; Wan, J.; He, H.W.
    Synthesis and antifungal activity of 5-iodo-1,4-disubstituted-1,2,3-triazole derivatives as pyruvate dehydrogenase complex E1 inhibitors (2015), Bioorg. Med. Chem., 23, 1395-1401 .
    View publication on PubMed
Search for more literature for 1.2.1.104

Inhibitors

Inhibitors Comment Organism Structure
4-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methoxy)benzonitrile exhibits very good enzyme-selective inhibition of PDH-E1 between pig heart and Escherichia coli and activity against Rhizoctonia solani and Botrytis cinerea even at 12.5 lg/ml Escherichia coli
5-((4-((4-bromophenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine exhibits activity against Rhizoctonia solani and Botrytis cinerea even at 12.5 lg/ml Escherichia coli
5-((4-((4-chloro-3-methylphenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
-
 Escherichia coli
5-((4-((4-chlorophenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine exhibits activity against Rhizoctonia solani even at 12.5 lg/ml and almost 5.5 times more inhibitory potency against Botryttis cinerea than pyrimethanil Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
pyruvate + CoA + oxidized 2,6-dichlorophenolindophenol
-
 Escherichia coli acetyl-CoA + CO2 + reduced 2,6-dichlorophenolindophenol
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0042
-
 isolated E1 component, pH 6.5, 37°C Escherichia coli 5-((4-((4-bromophenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
0.0051
-
 isolated E1 component, pH 6.5, 37°C Escherichia coli 5-((4-((4-chloro-3-methylphenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
0.0101
-
 isolated E1 component, pH 6.5, 37°C Escherichia coli 4-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methoxy)benzonitrile
0.0118
-
 isolated E1 component, pH 6.5, 37°C Escherichia coli 5-((4-((4-chlorophenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine