2.3.1.157 (1R,2R)-2-[[2,4-dimethoxy-5-(1,2,3,4-tetrahydroquinolin-2-ylsulfonyl)phenyl]carbamoyl]-3-methylcyclopropanecarboxylic acid - 15250 2.3.1.157 (1R,2R)-2-[[4-hydroxy-2-methoxy-5-(1,2,3,4-tetrahydroquinolin-2-ylsulfonyl)phenyl]carbamoyl]-3-methylcyclopropanecarboxylic acid - 15257 2.3.1.157 (1R,2R)-2-[[5-(acridin-10(9H)-ylsulfonyl)-2,4-dimethoxyphenyl]carbamoyl]-3-methylcyclopropanecarboxylic acid - 15249 2.3.1.157 (1R,2R)-2-[[5-(acridin-10(9H)-ylsulfonyl)-4-hydroxy-2-methoxyphenyl]carbamoyl]-3-methylcyclopropanecarboxylic acid - 15256 2.3.1.157 (2E)-4-([2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]amino)-4-oxobut-2-enoic acid - 10368 2.3.1.157 (2E)-4-[[2,4-dimethoxy-5-(10H-phenoxazin-10-ylsulfonyl)phenyl]amino]-4-oxobut-2-enoic acid - 215889 2.3.1.157 (4Z)-4-(4-benzyloxybenzylidene)-2-(naphthalen-2-yl)-1,3-oxazol-5(4H)-one a oxazolidine derivative that specifically inhibits GlmU. Administration to infected mice results in significant decrease in the bacillary load 208985 2.3.1.157 (5-[(E)-[(2,5-dimethylphenyl)imino]methyl]furan-2-yl)(hydroxy)oxoammonium 0.1 mM, 93.82% inhibition, competitive inhibition versus acetyl-CoA, uncompetitive inhibition versus glucose 1-phosphate 245399 2.3.1.157 (5-[(E)-[(2,5-dimethylphenyl)imino]methyl]furan-2-yl)(hydroxy)oxoammonium - 245399 2.3.1.157 (5E)-1-(3,5-dimethylphenyl)-5-(furan-2-ylmethylidene)pyrimidine-2,4,6(1H,3H,5H)-trione uncompetitive versus acetyl-CoA and alpha-D-glucosamine 1-phosphate, inhibits GlmU enzyme acetyltransferase activity 216059 2.3.1.157 (5Z)-2-imino-5-[(2E)-3-(5-nitrofuran-2-yl)prop-2-en-1-ylidene]-1,3-thiazolidin-4-one competitive versus acetyl-CoA, uncompetitive versus alpha-D-glucosamine 1-phosphate, specificly inhibits GlmU acetyltransferase activity and also exhibits whole cell activity against drug susceptible as well as drug resistant Mycobacterium tuberculosis. The compound also exhibits increased anti-tuberculois activity when tested in combination with rifampicin, isoniazid and ethambutol, but is cytotoxxic for the eukaryotic cell line; specific inhibition of acetyltransferase activity, competitive with respect to acetyl-CoA. Compound also exhibits whole cell activity against drug susceptible as well as drug resistant Mycobacterium tuberculosis and increased anti-TB activity when tested in combination with rifampicin, isoniazid and ethambutol. Compound is cytotoxic to eukaryotic cell line 208987 2.3.1.157 (5Z)-5-(furan-3-ylmethylidene)-1-(4-methoxyphenyl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione uncompetitive versus acetyl-CoA and alpha-D-glucosamine 1-phosphate, inhibits GlmU enzyme acetyltransferase activity 216061 2.3.1.157 (E)-N-(2,5-dimethylphenyl)-1-(5-nitrofuran-2-yl)methanimine specific inhibitor, 93.82% inhibition at 0.1 mM 217059 2.3.1.157 (E)-N-(2,5-dimethylphenyl)-1-(5-nitrofuran-2-yl)methanimine - 217059 2.3.1.157 (E)-N-(2-fluoro-5-nitrophenyl)-1-(5-nitrofuran-2-yl)methanimine specific inhibitor, 97.47% inhibition at 0.1 mM 217058 2.3.1.157 (E)-N-(2-fluoro-5-nitrophenyl)-1-(5-nitrofuran-2-yl)methanimine - 217058 2.3.1.157 1-(2-[[([5-[(3-carboxypropanoyl)amino]-2,4-dimethoxyphenyl]sulfonyl)amino]methyl]phenyl)piperidine-4-carboxylic acid - 10396 2.3.1.157 1-butyl-2-[(E)-2-(5-nitrofuran-2-yl)ethenyl]-1H-benzimidazole unspecific inhibitor, 84.26% inhibition at 0.1 mM 216157 2.3.1.157 1-[2,4-dimethoxy-5-(10H-phenoxazin-10-ylsulfonyl)phenylamino]-2-(-4-pyridyl)-1-ethanone commercial inhibitor 256633 2.3.1.157 1-[2,4-dimethoxy-5-(10H-phenoxazin-10-ylsulfonyl)phenylamino]-2-(4-pyridyl)-1-ethanone - 217746 2.3.1.157 2'-[[([5-[(3-carboxypropanoyl)amino]-2,4-dimethoxyphenyl]sulfonyl)amino]methyl]biphenyl-4-carboxylic acid - 12204 2.3.1.157 2-(2-cyanopyridin-4-yl)-N-[2,4-dimethoxy-5-(1,2,3,4-tetrahydroquinolin-2-ylsulfonyl)phenyl]acetamide - 15254 2.3.1.157 2-([2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]amino)-2-oxoethyl acetate - 10367 2.3.1.157 2-amino-2,3-dideoxy-3-fluoro-alpha-D-glucopyranosyl phosphate - 28699 2.3.1.157 2-nitro-5-thiocyanatobenzoic acid 0.5 mM, 5% residual activity 209793 2.3.1.157 2-Nitro-5-thiocyanobenzoic acid - 10489 2.3.1.157 3-fluoro-N-[1-(2-methylpropanoyl)-1,2,3,4-tetrahydroquinolin-6-yl]benzene-1-sulfonamide 0.1 mM, 82.87% inhibition, competitive inhibition versus acetyl-CoA, uncompetitive inhibition versus glucose 1-phosphate 245857 2.3.1.157 3-fluoro-N-[1-(2-methylpropanoyl)-1,2,3,4-tetrahydroquinolin-6-yl]benzene-1-sulfonamide - 245857 2.3.1.157 3-fluoro-N-[1-(2-methylpropanoyl)-1,2,3,4-tetrahydroquinolin-6-yl]benzenesulfonamide specific inhibitor, 82.87% inhibition at 0.1 mM 208983 2.3.1.157 3-fluoro-N-[1-(2-methylpropanoyl)-1,2,3,4-tetrahydroquinolin-6-yl]benzenesulfonamide - 208983 2.3.1.157 3-fluoro-N-[1-(2-methylpropanoyl)-1,2,3,4-tetrahydroquinolin-6-yl]benzenesulfonamide 0.1 mM, 83% inhibition of acetyltransferase activity of GlmU; 82.9% inhibition at 0.1 mM 208983 2.3.1.157 3-hydrazinylquinoline-2-thiol 93% inhibition at 0.1 mM, competitive with AcCoA and uncompetitive with alpha-D-glucosamine 1-phosphate. Antibacterial activity of the compound corelates with GlmU inhibition; specific inhibitor, 92.68% inhibition at 0.1 mM 208982 2.3.1.157 3-hydrazinylquinoline-2-thiol - 208982 2.3.1.157 3-hydrazinylquinoline-2-thiol 0.1 mM, 92.68% inhibition, competitive inhibition versus acetyl-CoA, uncompetitive inhibition versus glucose 1-phosphate 208982 2.3.1.157 3-[(2,4-dimethoxyphenyl)amino]-4-phenylcyclobut-3-ene-1,2-dione 40.0% inhibition at 0.1 mM 216336 2.3.1.157 4-(4-(benzyloxy)benzylidene)-2-(naphthalen-1-yl)oxazol-5(4H)-one i.e. Oxa33, syntesis of a specific GlmU inhibitor, molecular docking study, the inhibitor binds to an allosteric site of the uridyltransferase domain., overview. Oxa33 fails to inhibit cell growth even at concentrations as high as 0.150 mM 217747 2.3.1.157 4-([2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]amino)-4-oxobutanoic acid - 10369 2.3.1.157 4-([2,4-dimethoxy-5-[naphthalen-2-yl(phenyl)sulfamoyl]phenyl]amino)-4-oxobutanoic acid - 15245 2.3.1.157 4-([4-hydroxy-2-methoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]amino)-4-oxobutanoic acid - 10363 2.3.1.157 4-([5-[(4-aminophenyl)(phenyl)sulfamoyl]-2,4-dimethoxyphenyl]amino)-4-oxobutanoic acid - 5446 2.3.1.157 4-([5-[bis(4-methylphenyl)sulfamoyl]-2,4-dimethoxyphenyl]amino)-4-oxobutanoic acid - 15244 2.3.1.157 4-[(2,4-dimethoxy-5-[[2-(piperidin-1-yl)benzyl]sulfamoyl]phenyl)amino]-4-oxobutanoic acid - 10393 2.3.1.157 4-[(5-[[2-(4-[[(carboxyacetyl)oxy]methyl]piperidin-1-yl)benzyl]sulfamoyl]-2,4-dimethoxyphenyl)amino]-4-oxobutanoic acid - 10395 2.3.1.157 4-[2-([2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]amino)-2-oxoethoxy]benzoic acid - 10372 2.3.1.157 4-[[(2,6-dimethoxybenzoyl)oxy]imino]cyclohexa-2,5-dien-1-one competitive versus acetyl-CoA, noncompetitive versus alpha-D-glucosamine 1-phosphate, specificly inhibits GlmU acetyltransferase activity and also exhibits whole cell activity against drug susceptible as well as drug resistant Mycobacterium tuberculosis. The compound also exhibits increased anti-tuberculois activity when tested in combination with rifampicin, isoniazid and ethambutol; specific inhibition of acetyltransferase activity, competitive with respect to acetyl-CoA. Compound also exhibits whole cell activity against drug susceptible as well as drug resistant Mycobacterium tuberculosis and increased anti-TB activity when tested in combination with rifampicin, isoniazid and ethambutol 208986 2.3.1.157 4-[[2,4-dimethoxy-5-(10H-phenothiazin-10-ylsulfonyl)phenyl]amino]-4-oxobutanoic acid - 15246 2.3.1.157 4-[[2,4-dimethoxy-5-(10H-phenoxazin-10-ylsulfonyl)phenyl]amino]-4-oxobutanoic acid - 5069 2.3.1.157 4-[[2,4-dimethoxy-5-(10H-phenoxazin-10-ylsulfonyl)phenyl]amino]-4-oxobutanoic acid substrate inhibition, competitive versus N-[2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]acetamide 5069 2.3.1.157 4-[[4-hydroxy-2-methoxy-5-(1,2,3,4-tetrahydroquinolin-2-ylsulfonyl)phenyl]amino]-4-oxobutanoic acid - 15255 2.3.1.157 4-[[5-(dibenzo[b,f][1,4]oxazepin-10(11H)-ylsulfonyl)-2,4-dimethoxyphenyl]amino]-4-oxobutanoic acid - 15247 2.3.1.157 4-[[5-(diphenylsulfamoyl)-2,4-dimethoxyphenyl]amino]-4-oxobutanoic acid - 15243 2.3.1.157 4-[[5-(diphenylsulfamoyl)-2,4-dimethoxyphenyl]amino]-4-oxobutanoic acid pH and temperature not specified in the publication 15243 2.3.1.157 4-[[5-([2-[4-(carboxymethyl)piperidin-1-yl]benzyl]sulfamoyl)-2,4-dimethoxyphenyl]amino]-4-oxobutanoic acid - 10397 2.3.1.157 4-[[5-([2-[4-(hydroxymethyl)piperidin-1-yl]benzyl]sulfamoyl)-2,4-dimethoxyphenyl]amino]-4-oxobutanoic acid - 10394 2.3.1.157 5,5'-dithiobis-(2-nitrobenzoic acid) 0.1 mM, 33% residual activity 2053 2.3.1.157 5,7-dichloro-2-hydrazinylquinolin-8-ol 98% inhibition at 0.1 mM, competitive with AcCoA and uncompetitive with alpha-D-glucosamine 1-phosphate. Antibacterial activity of the compound corelates with GlmU inhibition; specific inhibitor, 98.25% inhibition at 0.1 mM 208981 2.3.1.157 5,7-dichloro-2-hydrazinylquinolin-8-ol - 208981 2.3.1.157 5,7-dichloro-2-hydrazinylquinolin-8-ol 0.1 mM, 98.25% inhibition, competitive inhibition versus acetyl-CoA, uncompetitive inhibition versus glucose 1-phosphate 208981 2.3.1.157 5-(1,2-oxazol-5-yl)-N-(pyridin-3-ylmethyl)furan-2-sulfonamide 44.7% inhibition at 0.1 mM 216583 2.3.1.157 6-chloro-N-[3-(methylsulfanyl)phenyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide unspecific inhibitor, 68.69% inhibition at 0.1 mM 208984 2.3.1.157 6-chloro-N-[3-(methylsulfanyl)phenyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide 0.1 mM, 69% inhibition of acetyltransferase activity of GlmU. Molecular dynamics simulation and binding site analysis; 68.7% inhibition at 0.1 mM 208984 2.3.1.157 6-chloro-N-[3-(methylsulfanyl)phenyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide 0.1 mM, 68.69% inhibition, competitive inhibition versus acetyl-CoA, uncompetitive inhibition versus glucose 1-phosphate 208984 2.3.1.157 6-chloro-N-[3-(methylsulfanyl)phenyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide - 208984 2.3.1.157 alpha-D-glucosamine 1-phosphate substrate inhibition, competitive versus N-[2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]acetamide 3255 2.3.1.157 butanoyl-CoA - 802 2.3.1.157 Ca2+ 2 mM, inhibits D-glucosamine-1-phosphate N-acetyltransferase activity 15 2.3.1.157 Co2+ 2 mM, inhibits D-glucosamine-1-phosphate N-acetyltransferase activity 23 2.3.1.157 CoA - 18 2.3.1.157 crotonyl-CoA - 406 2.3.1.157 D-galactosamine 1-phosphate - 113252 2.3.1.157 D-glucosamine 6-phosphate - 501 2.3.1.157 D-glucose 1-phosphate - 672 2.3.1.157 dicumarol uncompetitively inhibits acetyl CoA and shows mixed-type inhibition for glucosamine-1-phosphate. Dicumarol also exhibits inhibitory effects on several clinically sensitive Mycobacterium tuberculosis strains and drug-resistant strains, with a range of MIC value of 6.25 to more than 100 mg/ml. Dicumarol increases the sensitivity of anti-tuberculosis drugs (isoniazid and rifampicin) when dicumarol is present at a low concentration 15728 2.3.1.157 DTNB - 554 2.3.1.157 EDTA - 21 2.3.1.157 ethyl (2-[(Z)-[2-(ethylsulfanyl)-5-oxo-1,3-thiazol-4(5H)-ylidene]methyl]phenoxy)acetate 45.3% inhibition at 0.1 mM 216782 2.3.1.157 ethyl-CoA - 247220 2.3.1.157 iodoacetamide - 67 2.3.1.157 isobutanoyl-CoA - 15797 2.3.1.157 malonyl-CoA - 76 2.3.1.157 methyl 2-[([[5-(acetylamino)-2,4-dimethoxyphenyl]sulfonyl]amino)methyl]benzoate - 10390 2.3.1.157 Mg2+ 2 mM, inhibits D-glucosamine-1-phosphate N-acetyltransferase activity 6 2.3.1.157 Mn2+ 2 mM, inhibits D-glucosamine-1-phosphate N-acetyltransferase activity 11 2.3.1.157 additional information high throughput inhibitor screening for inhibition of the acetyltransferase domain of GlmU by a arylsulfonamide series 2 2.3.1.157 additional information inhibitor synthesis and inhibition potencies, overview 2 2.3.1.157 additional information inhibitor synthesis and inhibition potencies, MIC values, overview 2 2.3.1.157 additional information inhibitor synthesis and inhibition potencies, MIC values, overview; inhibitor synthesis and inhibition potencies, overview 2 2.3.1.157 additional information inhibitor synthesis, detailed overview. No inhibition of GlmU by methyl 2-amino-2-deoxyl-alpha-D-glucopyranoside 6-phosphate, methyl 2-amino-2-deoxyl-beta-D-glucopyranoside 6-phosphate, and 2-azido-2-deoxy-alpha-D-glucopyranosyl phosphate even at high concentrations 2 2.3.1.157 additional information inhibitor design from enzyme structure, analysis of antimicrobial compounds mediating their growth inhibitory effects specifically via GlmU, antimicrobial properties of sulfonamide inhibitors of GlmU acetyl transferase, overview 2 2.3.1.157 additional information modelling of competitive and uncompetitive inhibition of Rxn-1 by substrates/products, overview 2 2.3.1.157 additional information residues Tyr311, Lys337 and Lys340 plus C-terminal 11-residue region of the ST0452 protein enhance its GalN-1-P AcTase activity and suppress its GlcN-1-P AcTase activity, this function might be lost in bacterial enzymes 2 2.3.1.157 additional information ligand- and structure-guided screening of a compound library for inhibitors selective for the enzyme's acetyltransferase activity, quantitative two- and three-dimensional structure-activity relationship modelling, overview. Analysis of cytotoxicity of the inhibitors 2 2.3.1.157 additional information ligand- and structure-guided screening of a compound library for inhibitors selective for the enzyme's acetyltransferase activity, molecular docking and quantitative two- and three-dimensional structure-activity relationship modelling,, structure-function analysis, overview 2 2.3.1.157 additional information high-throughput screen identifies small molecule inhibitors targeting acetyltransferase activity of Mycobacterium tuberculosis GlmU, molecular docking studies, overview 2 2.3.1.157 N-(2,4-dimethoxy-5-[[2-(piperidin-1-yl)benzyl]sulfamoyl]phenyl)acetamide - 10391 2.3.1.157 N-(2,5-dimethoxyphenyl)-N-(phenylsulfonyl)glycine 42.01% inhibition at 0.1 mM 216866 2.3.1.157 N-(3-chlorophenyl)-2-methoxy-5-(2-methyl-1,3-oxazol-5-yl)benzenesulfonamide 406% inhibition at 0.1 mM 216876 2.3.1.157 N-(5-chloro-2-methoxyphenyl)-N-(phenylsulfonyl)glycine 45.15% inhibition at 0.1 mM 216940 2.3.1.157 N-([2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]carbamothioyl)glycine - 10365 2.3.1.157 N-([2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]carbamoyl)glycine - 10366 2.3.1.157 N-acetylglucosamine-1-phosphate acetyltransferase activity inhibited by its reaction product 31976 2.3.1.157 N-ethylmaleimide - 49 2.3.1.157 N-[2,4-dimethoxy-5-(1,2,3,4-tetrahydroquinolin-2-ylsulfonyl)phenyl]-2-(2-fluoropyridin-4-yl)acetamide - 15252 2.3.1.157 N-[2,4-dimethoxy-5-(1,2,3,4-tetrahydroquinolin-2-ylsulfonyl)phenyl]-3-(2H-tetrazol-5-yl)propanamide - 15248 2.3.1.157 N-[2,4-dimethoxy-5-(10H-phenoxazin-10-ylsulfonyl)phenyl]-2-(pyridin-4-yl)acetamide - 216958 2.3.1.157 N-[2,4-dimethoxy-5-(10H-phenoxazine-10-sulfonyl)phenyl]-2-(pyridin-4-yl)acetamide - 246770 2.3.1.157 N-[2,4-dimethoxy-5-(phenylsulfamoyl)phenyl]acetamide - 10375 2.3.1.157 N-[2,4-dimethoxy-5-(piperidin-1-ylsulfonyl)phenyl]acetamide - 10380 2.3.1.157 N-[2,4-dimethoxy-5-[(2-methoxybenzyl)sulfamoyl]phenyl]acetamide - 10387 2.3.1.157 N-[2,4-dimethoxy-5-[(2-methyl-2,3-dihydro-1H-indol-1-yl)sulfonyl]phenyl]acetamide the inhibitor binds at the C-terminal domain of GlmU engaging the A, B and C subunits of the trimer 10364 2.3.1.157 N-[2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]-2-(pyridin-4-ylsulfanyl)acetamide - 10371 2.3.1.157 N-[2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]acetamide - 4745 2.3.1.157 N-[2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]benzamide - 10374 2.3.1.157 N-[2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]methanesulfonamide - 10373 2.3.1.157 N-[2,4-dimethoxy-5-[(2-methylpyrrolidin-1-yl)sulfonyl]phenyl]acetamide - 10379 2.3.1.157 N-[2,4-dimethoxy-5-[(3-methylphenyl)sulfamoyl]phenyl]acetamide - 10385 2.3.1.157 N-[2,4-dimethoxy-5-[(4-methylphenyl)sulfamoyl]phenyl]acetamide - 10386 2.3.1.157 N-[2,4-dimethoxy-5-[methyl(phenyl)sulfamoyl]phenyl]acetamide - 4746 2.3.1.157 N-[2,4-dimethoxy-5-[phenyl(propan-2-yl)sulfamoyl]phenyl]acetamide - 10376 2.3.1.157 N-[5-(acridin-10(9H)-ylsulfonyl)-2,4-dimethoxyphenyl]-2-(2-fluoropyridin-4-yl)acetamide - 15253 2.3.1.157 N-[5-(acridin-10(9H)-ylsulfonyl)-2,4-dimethoxyphenyl]-2-(pyridin-4-yl)acetamide - 15251 2.3.1.157 N-[5-(dimethylsulfamoyl)-2,4-dimethoxyphenyl]acetamide - 10381 2.3.1.157 N-[5-([2-[4-(hydroxymethyl)piperidin-1-yl]benzyl]sulfamoyl)-2,4-dimethoxyphenyl]acetamide - 10392 2.3.1.157 N-[5-[(1,3-benzodioxol-5-ylmethyl)sulfamoyl]-2,4-dimethoxyphenyl]acetamide - 10388 2.3.1.157 N-[5-[(2-bromobenzyl)sulfamoyl]-2,4-dimethoxyphenyl]acetamide - 10389 2.3.1.157 N-[5-[(2-fluorophenyl)sulfamoyl]-2,4-dimethoxyphenyl]acetamide - 10384 2.3.1.157 N-[5-[(3-fluorophenyl)sulfamoyl]-2,4-dimethoxyphenyl]acetamide - 10383 2.3.1.157 N-[5-[(4-fluorophenyl)sulfamoyl]-2,4-dimethoxyphenyl]acetamide - 10382 2.3.1.157 N-[5-[butyl(propan-2-yl)sulfamoyl]-2,4-dimethoxyphenyl]acetamide - 10378 2.3.1.157 N-[5-[ethyl(2-methylphenyl)sulfamoyl]-2,4-dimethoxyphenyl]acetamide - 10377 2.3.1.157 p-hydroxymercuribenzoate - 98 2.3.1.157 terreic acid isolated from Aspergillus terreus, inhibits the acetyltransferase activity of Escherichia coli GlmU. The inhibition mode is competitive with acetyl-CoA and uncompetitive with alpha-D-glucosamine 1-phosphate. Terreic acid is cytotoxic against Escherichia coli strain ATCC 25922 and inhibit growth of biofilms. Molecular docking and binding structure, and cytotoxic effects, overview; isolated from Aspergillus terreus, inhibits the acetyltransferase domain. Terreic acid is competitive with acetyl-CoA and uncompetitive with alpha-D-glucosamine 1-phosphate and exhibits concentration-dependent killing of Escherichia coli ATCC 25922 up to 4-times minimum inhibitory concentration and inhibits the growth of biofilms generated by Escherichia coli 15315 2.3.1.157 terreic acid terreic acid inhibits the glucosamine-1-phosphate-acetyltransferase activity of the bifunctional enzyme. Mode of inhibition studies reveal that terreic acid is competitive with AcCoA and uncompetitive with GlcN-1-phosphate. It also exhibits concentration-dependent killing of Escherichia coli strain ATCC 25922 and inhibits the growth of biofilms generated by Escherichia coli. GlmU acetyltransferase is a molecular target of terreic acid, resulting in its antibacterial activity. Terreic acid is isolated from Aspergillus terreus strain MRCJ-356. Molecular modeling, MIC value 15315 2.3.1.157 terreic acid terreic acid inhibits the glucosamine-1-phosphate-acetyltransferase activity of the bifunctional enzyme. Mode of inhibition studies reveal that terreic acid is competitive with AcCoA and uncompetitive with GlcN-1-phosphate. It also exhibits concentration-dependent killing of Escherichia coli strain ATCC 25922 and inhibits the growth of biofilms generated by Escherichia coli. GlmU acetyltransferase is a molecular target of terreic acid, resulting in its antibacterial activity. Terreic acid is isolated from Aspergillus terreus strain MRCJ-356. Molecular modeling 15315 2.3.1.157 UDP-MurNAc 1 mM, relative enzyme activity 2% 49468 2.3.1.157 Zn2+ 2 mM, inhibits D-glucosamine-1-phosphate N-acetyltransferase activity 14 2.3.1.157 [2-([2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]amino)-2-oxoethoxy]acetic acid - 12203 2.3.1.157 [4-fluoro-3-[(E)-([5-[hydroxy(oxo)azaniumyl]furan-2-yl]methylidene)amino]phenyl](hydroxy)oxoammonium 0.1 mM, 97.47% inhibition, competitive inhibition versus acetyl-CoA, uncompetitive inhibition versus glucose 1-phosphate 246987 2.3.1.157 [4-fluoro-3-[(E)-([5-[hydroxy(oxo)azaniumyl]furan-2-yl]methylidene)amino]phenyl](hydroxy)oxoammonium - 246987 2.3.1.157 [5-[(E)-2-(1-butyl-1H-benzimidazol-2-yl)ethenyl]furan-2-yl](hydroxy)oxoammonium 0.1 mM, 84.26% inhibition, competitive inhibition versus acetyl-CoA, uncompetitive inhibition versus glucose 1-phosphate 246996 2.3.1.157 [5-[(E)-2-(1-butyl-1H-benzimidazol-2-yl)ethenyl]furan-2-yl](hydroxy)oxoammonium - 246996 2.3.1.157 [[2-([2,4-dimethoxy-5-[(2-methyl-3,4-dihydroquinolin-1(2H)-yl)sulfonyl]phenyl]amino)-2-oxoethyl]sulfanyl]acetic acid - 10370