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Literature summary extracted from

  • Xiao, Z.P.; Ouyang, H.; Wang, X.D.; Lv, P.C.; Huang, Z.J.; Yu, S.R.; Yi, T.F.; Yang, Y.L.; Zhu, H.L.
    4-Alkoxy-3-arylfuran-2(5H)-ones as inhibitors of tyrosyl-tRNA synthetase: Synthesis, molecular docking and antibacterial evaluation (2011), Bioorg. Med. Chem., 19, 3884-3891.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.1.1.1 3-(3,4-dichlorophenyl)-4-(2-(4-methylpiperazin-1-yl)ethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-(3,4-difluorophenyl)-4-(2-(piperidin-1-yl)ethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-(3,4-dimethoxyphenyl)-4-(2-(4-methylpiperazin-1-yl)ethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-(3,4-dimethoxyphenyl)-4-(2-(piperidin-1-yl)ethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-(3-bromophenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-(3-chlorophenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-(3-hydroxyphenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-(3-methoxyphenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-(4-bromophenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-(4-chlorophenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-(4-hydroxyphenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one replacement of the morpholine-ring in the side chain of the compound with a substituent containing more hydrophilic groups is probably more suitable for further modification. Most potent agent against Staphylococcus aureus ATCC 25923 with MIC50 value of 0.00023 mg/ml Staphylococcus aureus
6.1.1.1 3-(4-methoxyphenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-phenyl-4-(2-(piperidin-1-yl)ethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-phenyl-4-(2-(propylamino)ethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 3-phenyl-4-(2-(pyrrolidin-1-yl)ethoxy)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 4-(2-(2-(4-nitrophenyl)hydrazinyl)ethoxy)-3-phenylfuran-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 4-(2-(4-methylpiperazin-1-yl)ethoxy)-3-phenylfuran-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 4-(2-(benzylamino)ethoxy)-3-phenylfuran-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 4-(2-(butylamino)ethoxy)-3-phenylfuran-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 4-(2-(cyclohexylamino)ethoxy)-3-(3,4-dimethoxyphenyl)furan-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 4-(2-(cyclohexylamino)ethoxy)-3-phenylfuran-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 4-(2-morpholinoethoxy)-3-phenylfuran-2(5H)-one
-
Staphylococcus aureus
6.1.1.1 additional information synthesis of a series of novel 4-alkoxy-3-arylfuran-2(5H)-ones as tyrosyl-tRNA synthetase inhibitors, binding model and structure-activity relationship, MIC50 values, overview Staphylococcus aureus

Organism

EC Number Organism UniProt Comment Textmining
6.1.1.1 Staphylococcus aureus
-
-
-
6.1.1.1 Staphylococcus aureus ATCC 25923
-
-
-

Synonyms

EC Number Synonyms Comment Organism
6.1.1.1 TyrRS
-
Staphylococcus aureus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
6.1.1.1 0.0001
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(4-hydroxyphenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
6.1.1.1 0.00062
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(4-chlorophenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
6.1.1.1 0.0024
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(4-bromophenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
6.1.1.1 0.0062
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 4-(2-morpholinoethoxy)-3-phenylfuran-2(5H)-one
6.1.1.1 0.0086
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 4-(2-(4-methylpiperazin-1-yl)ethoxy)-3-phenylfuran-2(5H)-one
6.1.1.1 0.0205
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(3-chlorophenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
6.1.1.1 0.0243
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(3-bromophenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
6.1.1.1 0.0256
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(3-hydroxyphenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
6.1.1.1 0.0291
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-phenyl-4-(2-(propylamino)ethoxy)furan-2(5H)-one
6.1.1.1 0.0328
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(4-methoxyphenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
6.1.1.1 0.0355
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-phenyl-4-(2-(pyrrolidin-1-yl)ethoxy)furan-2(5H)-one
6.1.1.1 0.0375
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(3-methoxyphenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one
6.1.1.1 0.0536
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-phenyl-4-(2-(piperidin-1-yl)ethoxy)furan-2(5H)-one
6.1.1.1 0.0719
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 4-(2-(butylamino)ethoxy)-3-phenylfuran-2(5H)-one
6.1.1.1 0.0874
-
pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 4-(2-(cyclohexylamino)ethoxy)-3-phenylfuran-2(5H)-one
6.1.1.1 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 4-(2-(benzylamino)ethoxy)-3-phenylfuran-2(5H)-one
6.1.1.1 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 4-(2-(2-(4-nitrophenyl)hydrazinyl)ethoxy)-3-phenylfuran-2(5H)-one
6.1.1.1 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 4-(2-(cyclohexylamino)ethoxy)-3-(3,4-dimethoxyphenyl)furan-2(5H)-one
6.1.1.1 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(3,4-dimethoxyphenyl)-4-(2-(piperidin-1-yl)ethoxy)furan-2(5H)-one
6.1.1.1 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(3,4-dimethoxyphenyl)-4-(2-(4-methylpiperazin-1-yl)ethoxy)furan-2(5H)-one
6.1.1.1 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(3,4-dichlorophenyl)-4-(2-(4-methylpiperazin-1-yl)ethoxy)furan-2(5H)-one
6.1.1.1 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus 3-(3,4-difluorophenyl)-4-(2-(piperidin-1-yl)ethoxy)furan-2(5H)-one