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Literature summary for 1.3.98.1 extracted from

  • Haque, T.S.; Tadesse, S.; Marcinkeviciene, J.; Rogers, M.J.; Sizemore, C.; Kopcho, L.M.; Amsler, K.; Ecret, L.D.; Zhan, D.L.; Hobbs, F.; Slee, A.; Trainor, G.L.; Stern, A.M.; Copeland, R.A.; Combs, A.P.
    Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase (2002), J. Med. Chem., 45, 4669-4678.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-(4-methyl-benzylamide) 5-phenylamide minimum inhibitory concentration 0.032 mg/ml Helicobacter pylori
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-(isobutyl-amide) minimum inhibitory concentration above 0.064 mg/ml Helicobacter pylori
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-[(4-carbamoyl-phenyl)-amide] minimum inhibitory concentration 0.008 mg/ml Helicobacter pylori
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-phenylamide 3-[(pyridin-3-ylmethyl)-amide] minimum inhibitory concentration 0.00025 mg/ml Helicobacter pylori
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-[(4-piperidin-1-yl-phenyl)-amide] 3-[(pyridin-3-ylmethyl)-amide] minimum inhibitory concentration 0.002 mg/ml Helicobacter pylori
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-(isobutyl-amide) 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] minimum inhibitory concentration 0.064 mg/ml Helicobacter pylori
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzhydryl-amide 5-benzylamide minimum inhibitory concentration above 0.032 mg/ml Helicobacter pylori
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] minimum inhibitory concentration 0.003 mg/ml Helicobacter pylori
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-benzylamide 3-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] minimum inhibitory concentration above 0.032 mg/ml Helicobacter pylori
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-phenylamide 3-[(pyridin-3-ylmethyl)-amide] minimum inhibitory concentration 0.0005 mg/ml Helicobacter pylori
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] 3-[(tetrahydro-furan-2-yl)-amide] minimum inhibitory concentration above 0.032 mg/ml Helicobacter pylori
N3-benzyl-1-(4-chlorophenyl)-N5-phenyl-1H-pyrazole-3,5-dicarboxamide minimum inhibitory concentration 0.000125 mg/ml Helicobacter pylori

Organism

Organism UniProt Comment Textmining
Helicobacter pylori
-
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000004
-
N3-benzyl-1-(4-chlorophenyl)-N5-phenyl-1H-pyrazole-3,5-dicarboxamide
-
Helicobacter pylori
0.000004
-
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-phenylamide 3-[(pyridin-3-ylmethyl)-amide]
-
Helicobacter pylori
0.000006
-
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-[(4-carbamoyl-phenyl)-amide]
-
Helicobacter pylori
0.000008
-
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-[(4-piperidin-1-yl-phenyl)-amide] 3-[(pyridin-3-ylmethyl)-amide]
-
Helicobacter pylori
0.000012
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-phenylamide 3-[(pyridin-3-ylmethyl)-amide]
-
Helicobacter pylori
0.000026
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide]
-
Helicobacter pylori
0.000032
-
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-(4-methyl-benzylamide) 5-phenylamide
-
Helicobacter pylori
0.000091
-
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-(isobutyl-amide)
-
Helicobacter pylori
0.000138
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-(isobutyl-amide) 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide]
-
Helicobacter pylori
0.000331
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] 3-[(tetrahydro-furan-2-yl)-amide]
-
Helicobacter pylori
0.0015
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-benzylamide 3-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide]
-
Helicobacter pylori
0.0024
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzhydryl-amide 5-benzylamide
-
Helicobacter pylori
0.05
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] above Helicobacter pylori
0.05
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-benzylamide 3-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] above Helicobacter pylori
0.05
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzhydryl-amide 5-benzylamide above Helicobacter pylori
0.05
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-(isobutyl-amide) 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] above Helicobacter pylori
0.05
-
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-[(4-carbamoyl-phenyl)-amide] above Helicobacter pylori
0.05
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] 3-[(tetrahydro-furan-2-yl)-amide] above Helicobacter pylori
0.05
-
N3-benzyl-1-(4-chlorophenyl)-N5-phenyl-1H-pyrazole-3,5-dicarboxamide above Helicobacter pylori
0.05
-
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-[(4-piperidin-1-yl-phenyl)-amide] 3-[(pyridin-3-ylmethyl)-amide] above Helicobacter pylori
0.05
-
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-(isobutyl-amide) above Helicobacter pylori
0.05
-
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-phenylamide 3-[(pyridin-3-ylmethyl)-amide] above Helicobacter pylori
0.05
-
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-(4-methyl-benzylamide) 5-phenylamide above Helicobacter pylori
0.05
-
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-phenylamide 3-[(pyridin-3-ylmethyl)-amide] above Helicobacter pylori