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Literature summary for 3.5.1.88 extracted from

  • Lv, F.; Chen, C.; Tang, Y.; Wei, J.; Zhu, T.; Hu, W.
    New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment (2016), Bioorg. Med. Chem. Lett., 26, 3714-3718 .
    View publication on PubMed
Search for more literature for 3.5.1.88

Inhibitors

Inhibitors Comment Organism Structure
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-(1H-pyrazol-3-yl)-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-(1H-pyrazol-3-yl)-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-(4-methyl-3-[[4-(pyridin-3-yl)pyrimidin-2-yl]amino]phenyl)-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-(4-methyl-3-[[4-(pyridin-3-yl)pyrimidin-2-yl]amino]phenyl)-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-(5-methyl-1,3-thiazol-2-yl)-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-(5-methyl-1,3-thiazol-2-yl)-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-[3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-[3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-[3-(pyridin-3-yl)phenyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-[3-(pyridin-3-yl)phenyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-[3-[(pyrimidin-2-yl)amino]phenyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-[3-[(pyrimidin-2-yl)amino]phenyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-[4-(pyridin-3-yl)pyrimidin-2-yl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-[4-(pyridin-3-yl)pyrimidin-2-yl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-[5-(pyridin-2-yl)-1,3,4-oxadiazol-2-yl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-N-[5-(pyridin-2-yl)-1,3,4-oxadiazol-2-yl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-N-(1H-benzimidazol-2-yl)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-N-(1H-benzimidazol-2-yl)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-N-(3-fluoropyridin-2-yl)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-N-(3-fluoropyridin-2-yl)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-N-(4-fluoropyridin-2-yl)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-N-(4-fluoropyridin-2-yl)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
(6S)-N-(5-tert-butyl-1,2-oxazol-3-yl)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Escherichia coli
(6S)-N-(5-tert-butyl-1,2-oxazol-3-yl)-5-[(2R)-2-[[formyl(hydroxy)amino]methyl]hexanoyl]-5-azaspiro[2.4]heptane-6-carboxamide
-
 Staphylococcus aureus
actinonin
-
 Escherichia coli
actinonin
-
 Staphylococcus aureus
GSK1322322
-
 Escherichia coli
GSK1322322
-
 Staphylococcus aureus
LBM415
-
 Escherichia coli
LBM415
-
 Staphylococcus aureus
additional information molecular docking and screening of designed small molecule ligands, a critical arginine residue in peptide deformylase for spiro cyclopropyl PDF inhibitor's extra hydrophobic binding is identified. Compund synthesis and structure confirmation by LC-MS, 1H NMR, 13C NMR, and HRMS. The compounds are evaluated through in vitro antibacterial activity assay, some are further subjected to in vivo rat pharmacokinetic assessment. Spiro cyclopropyl proline N-formyl hydroxylamines, and especially the bioisosteric azoles, are a promising class of PDF inhibitors Escherichia coli
additional information molecular docking and screening of designed small molecule ligands, a critical arginine residue in peptide deformylase for spiro cyclopropyl PDF inhibitor's extra hydrophobic binding is identified. Compund synthesis and structure confirmation by LC-MS, 1H NMR, 13C NMR, and HRMS. The compounds are evaluated through in vitro antibacterial activity assay, some are further subjected to in vivo rat pharmacokinetic assessment. Spiro cyclopropyl proline N-formyl hydroxylamines, and especially the bioisosteric azoles, are a promising class of PDF inhibitors Staphylococcus aureus

Organism

Organism UniProt Comment Textmining
Escherichia coli P0A6K3
-
-
Staphylococcus aureus P68826 MRSA
-

Synonyms

Synonyms Comment Organism
PDF
-
 Escherichia coli
PDF
-
 Staphylococcus aureus