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Literature summary for 5.1.1.3 extracted from

  • Geng, B.; Basarab, G.; Comita-Prevoir, J.; Gowravaram, M.; Hill, P.; Kiely, A.; Loch, J.; Macpherson, L.; Morningstar, M.; Mullen, G.; Osimboni, E.; Satz, A.; Eyermann, C.; Lundqvist, T.
    Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): Pyridodiazepine amines (2009), Bioorg. Med. Chem. Lett., 19, 930-936.
    View publication on PubMed
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Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with pyridodiazepine amine inhibitors Helicobacter pylori

Inhibitors

Inhibitors Comment Organism Structure
3-(3-chlorothiophen-2-yl)-5-(furan-2-yl)-N-methyl-3H-pyrido[2,3-e][1,4]diazepin-2-amine uncompetitive, inhibitor with improved solubility and reduced plasma protein binding, binds at the enzyme dimer interface Helicobacter pylori
5-(furan-2-yl)-N-methyl-3-(thiophen-2-yl)-3H-pyrido[2,3-e][1,4]diazepin-2-amine uncompetitive, inhibitor with improved solubility and reduced plasma protein binding, binds at the enzyme dimer interface Helicobacter pylori
N,8-dimethyl-5-phenyl-3-(thiophen-2-yl)-3H-pyrido[2,3-e][1,4]diazepin-2-amine uncompetitive, inhibitor with improved solubility and reduced plasma protein binding, binds at the enzyme dimer interface Helicobacter pylori
N-methyl-3,5-di(thiophen-2-yl)-3H-pyrido[2,3-e][1,4]diazepin-2-amine uncompetitive, inhibitor with improved solubility and reduced plasma protein binding, binds at the enzyme dimer interface Helicobacter pylori
N-methyl-5-(1H-pyrrol-3-yl)-3-(thiophen-2-yl)-3H-pyrido[2,3-e][1,4]diazepin-2-amine uncompetitive, inhibitor with improved solubility and reduced plasma protein binding, binds at the enzyme dimer interface Helicobacter pylori
N-methyl-5-phenyl-3-(thiophen-2-yl)-3H-pyrido[2,3-e][1,4]diazepin-2-amine uncompetitive, inhibitor with improved solubility and reduced plasma protein binding, binds at the enzyme dimer interface Helicobacter pylori

Organism

Organism UniProt Comment Textmining
Helicobacter pylori Q9ZLT0
-
-

Source Tissue

Source Tissue Comment Organism Textmining

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0006
-
-
 Helicobacter pylori N-methyl-5-(1H-pyrrol-3-yl)-3-(thiophen-2-yl)-3H-pyrido[2,3-e][1,4]diazepin-2-amine
0.0007
-
-
 Helicobacter pylori N-methyl-3,5-di(thiophen-2-yl)-3H-pyrido[2,3-e][1,4]diazepin-2-amine
0.0017
-
-
 Helicobacter pylori N,8-dimethyl-5-phenyl-3-(thiophen-2-yl)-3H-pyrido[2,3-e][1,4]diazepin-2-amine
0.002
-
-
 Helicobacter pylori 5-(furan-2-yl)-N-methyl-3-(thiophen-2-yl)-3H-pyrido[2,3-e][1,4]diazepin-2-amine
0.0022
-
-
 Helicobacter pylori N-methyl-5-phenyl-3-(thiophen-2-yl)-3H-pyrido[2,3-e][1,4]diazepin-2-amine
0.0028
-
-
 Helicobacter pylori 3-(3-chlorothiophen-2-yl)-5-(furan-2-yl)-N-methyl-3H-pyrido[2,3-e][1,4]diazepin-2-amine