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Literature summary for 1.1.1.86 extracted from

  • Wang, B.L.; Zhang, L.Y.; Liu, X.H.; Ma, Y.; Zhang, Y.; Li, Z.M.; Zhang, X.
    Synthesis, biological activities and SAR studies of new 3-substitutedphenyl-4-substituted benzylideneamino-1,2,4-triazole Mannich bases and bis-Mannich bases as ketol-acid reductoisomerase inhibitors (2017), Bioorg. Med. Chem. Lett., 27, 5457-5462 .
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
(2E)-1-[(2-fluorophenyl)(imino)methyl]-2-[(4-fluorophenyl)methylidene]-N-[(piperazin-1-yl)methyl]hydrazine-1-carbothioamide 0.2 mM, 82.04% inhibition Oryza sativa Japonica Group
(2E)-1-[(2-fluorophenyl)(imino)methyl]-2-[(4-fluorophenyl)methylidene]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 9.89% inhibition Oryza sativa Japonica Group
(2E)-1-[(2-fluorophenyl)(imino)methyl]-2-[(4-fluorophenyl)methylidene]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 11.75% inhibition Oryza sativa Japonica Group
(2E)-1-[(2-fluorophenyl)(imino)methyl]-N-[(piperazin-1-yl)methyl]-2-[[4-(trifluoromethyl)phenyl]methylidene]hydrazine-1-carbothioamide 0.2 mM, 69.3% inhibition Oryza sativa Japonica Group
(2E)-1-[(2-fluorophenyl)(imino)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]-2-[[4-(trifluoromethyl)phenyl]methylidene]hydrazine-1-carbothioamide 0.2 mM, 1.17% inhibition; 0.2 mM, 1.35% inhibition; 0.2 mM, 6.68% inhibition Oryza sativa Japonica Group
(2E)-1-[imino(phenyl)methyl]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]-2-[[4-(trifluoromethyl)phenyl]methylidene]hydrazine-1-carbothioamide 0.2 mM, 12.27% inhibition; 0.2 mM, 61.99% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-chlorophenyl)methylidene]-1-[(2-fluorophenyl)(imino)methyl]-N-[(piperazin-1-yl)methyl]hydrazine-1-carbothioamide 0.2 mM, 74.8% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-chlorophenyl)methylidene]-1-[(2-fluorophenyl)(imino)methyl]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 11.94% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-chlorophenyl)methylidene]-1-[(2-fluorophenyl)(imino)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 14.91% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-chlorophenyl)methylidene]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 30.59% inhibition; 0.2 mM, 51.84% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-chlorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[(piperazin-1-yl)methyl]hydrazine-1-carbothioamide 0.2 mM, 60.45% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-chlorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 28.54% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-chlorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 7.4% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-chlorophenyl)methylidene]-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-1-[(2-fluorophenyl)(imino)methyl]hydrazine-1-carbothioamide 0.2 mM, 23.95% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-chlorophenyl)methylidene]-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]hydrazine-1-carbothioamide 0.2 mM, 19.65% inhibition; 0.2 mM, 81.81% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-fluorophenyl)methylidene]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 7.72% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-fluorophenyl)methylidene]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 13.65% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-fluorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[(piperazin-1-yl)methyl]hydrazine-1-carbothioamide 0.2 mM, 72.01% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-fluorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 10.34% inhibition Oryza sativa Japonica Group
(2E)-2-[(4-fluorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide 0.2 mM, 10.14% inhibition Oryza sativa Japonica Group
(2E)-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-1-[(2-fluorophenyl)(imino)methyl]-2-[(4-fluorophenyl)methylidene]hydrazine-1-carbothioamide 0.2 mM, 75.66% inhibition Oryza sativa Japonica Group
(2E)-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-2-[(4-fluorophenyl)methylidene]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]hydrazine-1-carbothioamide 0.2 mM, 6.22% inhibition; 0.2 mM, 78.38% inhibition Oryza sativa Japonica Group
(2E)-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-2-[(4-fluorophenyl)methylidene]-1-[imino(phenyl)methyl]hydrazine-1-carbothioamide 0.2 mM, 8.19% inhibition Oryza sativa Japonica Group
1-cyano-cyclopropane-1-carboxylate
-
 Oryza sativa Japonica Group
cyclopropane-1,1-dicarboxylate 0.2 mM, 100% inhibition Oryza sativa Japonica Group
N-isopropyloxalyl hydroxamate 0.2 mM, 100% inhibition Oryza sativa Japonica Group

Organism

Organism UniProt Comment Textmining
Oryza sativa Japonica Group Q65XK0
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000903
-
 N-isopropyloxalyl hydroxamate pH and temperature not specified in the publication Oryza sativa Japonica Group
0.00038
-
 (2E)-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-1-[(2-fluorophenyl)(imino)methyl]-2-[(4-fluorophenyl)methylidene]hydrazine-1-carbothioamide pH and temperature not specified in the publication Oryza sativa Japonica Group
0.00275
-
 cyclopropane-1,1-dicarboxylate pH and temperature not specified in the publication Oryza sativa Japonica Group
0.00659
-
 (2E)-1-[(2-fluorophenyl)(imino)methyl]-2-[(4-fluorophenyl)methylidene]-N-[(piperazin-1-yl)methyl]hydrazine-1-carbothioamide pH and temperature not specified in the publication Oryza sativa Japonica Group
0.00846
-
 (2E)-1-[(2-fluorophenyl)(imino)methyl]-N-[(piperazin-1-yl)methyl]-2-[[4-(trifluoromethyl)phenyl]methylidene]hydrazine-1-carbothioamide pH and temperature not specified in the publication Oryza sativa Japonica Group
0.01975
-
 (2E)-2-[(4-chlorophenyl)methylidene]-1-[(2-fluorophenyl)(imino)methyl]-N-[(piperazin-1-yl)methyl]hydrazine-1-carbothioamide pH and temperature not specified in the publication Oryza sativa Japonica Group
0.03519
-
 (2E)-2-[(4-chlorophenyl)methylidene]-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]hydrazine-1-carbothioamide pH and temperature not specified in the publication Oryza sativa Japonica Group
0.0585
-
 1-cyano-cyclopropane-1-carboxylate pH and temperature not specified in the publication Oryza sativa Japonica Group