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Literature summary extracted from

  • Apfel, C.; Banner, D.W.; Bur, D.; Dietz, M.; Hubschwerlen, C.; Locher, H.; Marlin, F.; Masciadri, R.; Pirson, W.; Stalder, H.
    2-(2-Oxo-1,4-dihydro-2H-quinazolin-3-yl)- and 2-(2,2-dioxo-1,4-dihydro-2H-2lambda6-benzo[1,2,6]thiadiazin-3-yl)-N-hydrox y-acetamides as potent and selective peptide deformylase inhibitors (2001), J. Med. Chem., 44, 1847-1852.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.5.1.88 2-(1-benzyl-5-chloro-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide IC50: 0.002 mM Escherichia coli
3.5.1.88 2-(1-butyl-5-chloro-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide IC50: 0.00059 mM Escherichia coli
3.5.1.88 2-(2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide IC50: 0.00076 mM Escherichia coli
3.5.1.88 2-(5-bromo-1-cyclopropyl-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide IC50: 0.000069 mM Escherichia coli
3.5.1.88 2-(5-bromo-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide IC50: 0.000098 mM Escherichia coli
3.5.1.88 2-(5-bromo-2-oxo-1,4-dihydroquinazolin-3(2H)-yl)-N-hydroxyacetamide IC50: 0.000049 mM Escherichia coli
3.5.1.88 2-(5-chloro-1-cyclopropyl-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide IC50: 0.00011 mM Escherichia coli
3.5.1.88 2-(5-chloro-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide inhibitor shows good selectivity for peptide deformylase over several endoproteases including matrix metalloproteases, however it shows only weak antibacterial activity. IC50: 0.00012 mM Escherichia coli
3.5.1.88 2-(5-chloro-2-oxo-1,4-dihydroquinazolin-3(2H)-yl)-N-hydroxyacetamide inhibitor shows good selectivity for peptide deformylase over several endoproteases including matrix metalloproteases, however it shows only weak antibacterial activity. IC50: 0.00031 mM Escherichia coli
3.5.1.88 2-(5-chloro-2-oxo-1,4-dihydroquinazolin-3(2H)-yl)acetohydrazide IC50: 0.027 mM Escherichia coli
3.5.1.88 2-(5-fluoro-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide IC50: 0.00087 mM Escherichia coli
3.5.1.88 2-(5-fluoro-2-oxo-1,4-dihydroquinazolin-3(2H)-yl)-N-hydroxyacetamide IC50: 0.00087 mM Escherichia coli
3.5.1.88 2-[2,2-dioxido-5-(trifluoromethyl)-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl]-N-hydroxyacetamide IC50: 0.00013 mM Escherichia coli
3.5.1.88 2-[5-chloro-2,2-dioxido-1-(3-phenylpropyl)-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl]-N-hydroxyacetamide IC50: 0.00029 mM Escherichia coli
3.5.1.88 N-hydroxy-2-(2-oxo-1,4-dihydroquinazolin-3(2H)-yl)acetamide IC50: 0.0029 mM Escherichia coli
3.5.1.88 N-hydroxy-2-[2-oxo-5-(trifluoromethyl)-1,4-dihydroquinazolin-3(2H)-yl]acetamide IC50: 0.00023 mM Escherichia coli

Organism

EC Number Organism UniProt Comment Textmining
3.5.1.88 Escherichia coli
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.5.1.88 formyl-Met-Ala-Ser + H2O
-
 Escherichia coli formate + Met-Ala-Ser
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.5.1.88 0.000049
-
 IC50: 0.000049 mM Escherichia coli 2-(5-bromo-2-oxo-1,4-dihydroquinazolin-3(2H)-yl)-N-hydroxyacetamide
3.5.1.88 0.000069
-
 IC50: 0.000069 mM Escherichia coli 2-(5-bromo-1-cyclopropyl-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide
3.5.1.88 0.000098
-
 IC50: 0.000098 mM Escherichia coli 2-(5-bromo-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide
3.5.1.88 0.00011
-
 IC50: 0.00011 mM Escherichia coli 2-(5-chloro-1-cyclopropyl-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide
3.5.1.88 0.00012
-
 inhibitor shows good selectivity for peptide deformylase over several endoproteases including matrix metalloproteases, however it shows only weak antibacterial activity. IC50: 0.00012 mM Escherichia coli 2-(5-chloro-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide
3.5.1.88 0.00013
-
 IC50: 0.00013 mM Escherichia coli 2-[2,2-dioxido-5-(trifluoromethyl)-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl]-N-hydroxyacetamide
3.5.1.88 0.00023
-
 IC50: 0.00023 mM Escherichia coli N-hydroxy-2-[2-oxo-5-(trifluoromethyl)-1,4-dihydroquinazolin-3(2H)-yl]acetamide
3.5.1.88 0.00029
-
 IC50: 0.00029 mM Escherichia coli 2-[5-chloro-2,2-dioxido-1-(3-phenylpropyl)-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl]-N-hydroxyacetamide
3.5.1.88 0.00031
-
 inhibitor shows good selectivity for peptide deformylase over several endoproteases including matrix metalloproteases, however it shows only weak antibacterial activity. IC50: 0.00031 mM Escherichia coli 2-(5-chloro-2-oxo-1,4-dihydroquinazolin-3(2H)-yl)-N-hydroxyacetamide
3.5.1.88 0.00059
-
 IC50: 0.00059 mM Escherichia coli 2-(1-butyl-5-chloro-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide
3.5.1.88 0.00076
-
 IC50: 0.00076 mM Escherichia coli 2-(2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide
3.5.1.88 0.00087
-
 IC50: 0.00087 mM Escherichia coli 2-(5-fluoro-2-oxo-1,4-dihydroquinazolin-3(2H)-yl)-N-hydroxyacetamide
3.5.1.88 0.00087
-
 IC50: 0.00087 mM Escherichia coli 2-(5-fluoro-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide
3.5.1.88 0.002
-
 IC50: 0.002 mM Escherichia coli 2-(1-benzyl-5-chloro-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl)-N-hydroxyacetamide
3.5.1.88 0.0029
-
 IC50: 0.0029 mM Escherichia coli N-hydroxy-2-(2-oxo-1,4-dihydroquinazolin-3(2H)-yl)acetamide
3.5.1.88 0.027
-
 IC50: 0.027 mM Escherichia coli 2-(5-chloro-2-oxo-1,4-dihydroquinazolin-3(2H)-yl)acetohydrazide