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Literature summary for 6.5.1.2 extracted from

  • Surivet, J.P.; Lange, R.; Hubschwerlen, C.; Keck, W.; Specklin, J.L.; Ritz, D.; Bur, D.; Locher, H.; Seiler, P.; Strasser, D.S.; Prade, L.; Kohl, C.; Schmitt, C.; Chapoux, G.; Ilhan, E.; Ekambaram, N.; Athanasiou, A.; Knezevic, A.; Sabato, D.; Chambovey, A.; Gaertner, M.; Enderlin, M.; Boehme, M.; Sipp, S.i.p.p.e.
    Structure-guided design, synthesis and biological evaluation of novel DNA ligase inhibitors with in vitro and in vivo anti-staphylococcal activity (2012), Bioorg. Med. Chem. Lett., 22, 6705-6711.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-amino-5-(2-hydroxyethyl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-5-(2-methoxyethyl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-5-(aminomethyl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-5-methyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-5-phenyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-5-[(3R)-3-aminopyrrolidin-1-yl]-6-bromo-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-(2-phenylethyl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-(hydroxymethyl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-(propan-2-yl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-benzyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-benzyl-7-chloro-5-methyl-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-bromo-5-(3-hydroxyazetidin-1-yl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-bromo-5-(4-hydroxypiperidin-1-yl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-bromo-5-[(2-hydroxyethyl)(methyl)amino]-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-bromo-5-[(3R)-3-hydroxypyrrolidin-1-yl]-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-bromo-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-bromo-7-cyclopentyl-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-bromo-7-tert-butyl-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-chloro-5-ethyl-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-cyclopentyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-cyclopropyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-ethenyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-ethyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-6-methyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-7-chloro-5-methyl-6-(prop-2-en-1-yl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-7-chloro-5-methyl-6-(pyridin-4-ylmethyl)-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
2-amino-7-[2-(benzyloxy)propan-2-yl]-6-bromo-1,8-naphthyridine-3-carboxamide
-
Escherichia coli
4-amino-6-(1H-benzimidazol-2-yl)pyridazin-3(2H)-one
-
Escherichia coli
7-methoxy-6-methylpteridine-2,4-diamine
-
Escherichia coli
tert-butyl 3-(7-amino-3-bromo-6-carbamoyl-1,8-naphthyridin-2-yl)azetidine-1-carboxylate
-
Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-

Synonyms

Synonyms Comment Organism
LigA
-
Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0003
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-bromo-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0003
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-bromo-7-tert-butyl-1,8-naphthyridine-3-carboxamide
0.0004
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-ethenyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0004
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-cyclopropyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0005
-
pH and temperature not specified in the publication Escherichia coli 2-amino-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0005
-
pH and temperature not specified in the publication Escherichia coli 2-amino-5-methyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0005
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-benzyl-7-chloro-5-methyl-1,8-naphthyridine-3-carboxamide
0.0005
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-bromo-7-cyclopentyl-1,8-naphthyridine-3-carboxamide
0.0005
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-methyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0005
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-(hydroxymethyl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0005
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-bromo-5-(3-hydroxyazetidin-1-yl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0006
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-ethyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0007
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-bromo-5-[(2-hydroxyethyl)(methyl)amino]-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0007
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-bromo-5-[(3R)-3-hydroxypyrrolidin-1-yl]-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0007
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-bromo-5-(4-hydroxypiperidin-1-yl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0008
-
pH and temperature not specified in the publication Escherichia coli 2-amino-7-chloro-5-methyl-6-(prop-2-en-1-yl)-1,8-naphthyridine-3-carboxamide
0.0008
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-(propan-2-yl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0008
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-benzyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.001
-
pH and temperature not specified in the publication Escherichia coli 2-amino-7-chloro-5-methyl-6-(pyridin-4-ylmethyl)-1,8-naphthyridine-3-carboxamide
0.001
-
pH and temperature not specified in the publication Escherichia coli 2-amino-5-[(3R)-3-aminopyrrolidin-1-yl]-6-bromo-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.001
-
value above, pH and temperature not specified in the publication Escherichia coli 2-amino-6-(2-phenylethyl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0025
-
pH and temperature not specified in the publication Escherichia coli 2-amino-5-(aminomethyl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0025
-
pH and temperature not specified in the publication Escherichia coli 2-amino-5-phenyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.0025
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-cyclopentyl-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.005
-
value above, pH and temperature not specified in the publication Escherichia coli 2-amino-7-[2-(benzyloxy)propan-2-yl]-6-bromo-1,8-naphthyridine-3-carboxamide
0.005
-
value above, pH and temperature not specified in the publication Escherichia coli tert-butyl 3-(7-amino-3-bromo-6-carbamoyl-1,8-naphthyridin-2-yl)azetidine-1-carboxylate
0.008
-
pH and temperature not specified in the publication Escherichia coli 2-amino-6-chloro-5-ethyl-1,8-naphthyridine-3-carboxamide
0.01
-
pH and temperature not specified in the publication Escherichia coli 2-amino-5-(2-methoxyethyl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.01
-
pH and temperature not specified in the publication Escherichia coli 2-amino-5-(2-hydroxyethyl)-7-(trifluoromethyl)-1,8-naphthyridine-3-carboxamide
0.025
-
pH and temperature not specified in the publication Escherichia coli 7-methoxy-6-methylpteridine-2,4-diamine
0.025
-
value above, pH and temperature not specified in the publication Escherichia coli 4-amino-6-(1H-benzimidazol-2-yl)pyridazin-3(2H)-one