Design and evaluation of azaindole-substituted N-hydroxypyridones as glyoxalase I inhibitors

We conducted a high throughput screening for glyoxalase I (GLO1) inhibitors and identified 4,6-diphenyl-N-hydroxypyridone as a lead compound. Using a binding model of the lead and public X-ray coordinates of GLO1 enzymes complexed with glutathione analogues, we designed 4-(7-azaindole)-substituted 6...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-12, Vol.22 (24), p.7486-7489
Hauptverfasser:	Chiba, Takashi, Ohwada, Jun, Sakamoto, Hiroshi, Kobayashi, Takamitsu, Fukami, Takaaki A., Irie, Machiko, Miura, Takaaki, Ohara, Kazuhiro, Koyano, Hiroshi
Format:	Artikel
Sprache:	eng
Schlagworte:	7-Azaindole Biological and medical sciences Crystallography, X-Ray Dose-Response Relationship, Drug Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Enzymes Glutathione Glyoxalase I (GLO1) high-throughput screening Humans Indole Indoles - chemistry Ionizing radiation Lactoylglutathione lyase Lactoylglutathione Lyase - antagonists & inhibitors Lactoylglutathione Lyase - metabolism Medical sciences Models, Molecular Molecular Structure N-Hydroxypyridone Pharmacology. Drug treatments Pyridones - chemical synthesis Pyridones - chemistry Pyridones - pharmacology screening Structure-Activity Relationship Structure-activity relationships Structure-based drug design (SBDD) Thermodynamics X-radiation X-ray crystallography X-ray diffraction
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