Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.5.1.9 extracted from

  • Serer, M.I.; Carrica, M.D.C.; Trappe, J.; Lopez Romero, S.; Bonomi, H.R.; Klinke, S.; Cerutti, M.L.; Goldbaum, F.A.
    A high-throughput screening for inhibitors of riboflavin synthase identifies novel antimicrobial compounds to treat brucellosis (2019), FEBS J., 286, 2522-2535 .
    View publication on PubMed
Search for more literature for 2.5.1.9

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli BL21(DE3) cells Brucella abortus

Inhibitors

Inhibitors Comment Organism Structure
(2-ethyl-5-oxo-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7-yl)methyl 3,4,5-triethoxybenzoate
-
 Brucella abortus
(2E)-3-(2,3-dimethoxyphenyl)-N-[4-methyl-2-(4-methylpiperazin-1-yl)quinolin-6-yl]prop-2-enamide
-
 Brucella abortus
2-(4-ethoxyphenyl)-N-[3-(piperidin-1-yl)propyl]imidazo[2,1-b][1,3]benzothiazole-7-carboxamide
-
 Brucella abortus
2-(4-methoxyphenyl)-N-[3-(piperidin-1-yl)propyl]imidazo[2,1-b][1,3]benzothiazole-7-carboxamide
-
 Brucella abortus
2-[ethyl(methyl)amino]ethyl 4-[(5-ethyl-4-oxo-4,5-dihydrothieno[3,2-c]quinoline-2-carbonyl)amino]benzoate
-
 Brucella abortus
5-[3-(propan-2-yl)-1H-pyrazol-5-yl]-3-(3,4,5-trimethoxyphenyl)-1,2,4-oxadiazole
-
 Brucella abortus
ethyl 5-(diethylcarbamoyl)-2-[2-(4-methoxyphenoxy)acetamido]-4-methylthiophene-3-carboxylate
-
 Brucella abortus
additional information a high-throughput screening for inhibitors of riboflavin synthase identifies antimicrobial compounds to treat brucellosis Brucella abortus
N-[3-(azepan-1-yl)propyl]-2-(4-methoxyphenyl)imidazo[2,1-b][1,3]benzothiazole-7-carboxamide
-
 Brucella abortus
N-[3-(diethylamino)propyl]-2-(4-ethoxyphenyl)imidazo[2,1-b][1,3]benzothiazole-7-carboxamide
-
 Brucella abortus
N-[3-(diethylamino)propyl]-2-(4-methylphenyl)imidazo[2,1-b][1,3]benzothiazole-7-carboxamide
-
 Brucella abortus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0024
-
 6,7-dimethyl-8-(1-D-ribityl)lumazine pH 7.5, 37°C Brucella abortus

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
69000
-
-
 Brucella abortus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2 6,7-dimethyl-8-(1-D-ribityl)lumazine Brucella abortus
-
 riboflavin + 4-(1-D-ribitylamino)-5-amino-2,6-dihydroxypyrimidine
-
 ?

Organism

Organism UniProt Comment Textmining
Brucella abortus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Brucella abortus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2 6,7-dimethyl-8-(1-D-ribityl)lumazine
-
 Brucella abortus riboflavin + 4-(1-D-ribitylamino)-5-amino-2,6-dihydroxypyrimidine
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00235
-
 pH 7.5, 37°C Brucella abortus 2-[ethyl(methyl)amino]ethyl 4-[(5-ethyl-4-oxo-4,5-dihydrothieno[3,2-c]quinoline-2-carbonyl)amino]benzoate
0.01912
-
 pH 7.5, 37°C Brucella abortus ethyl 5-(diethylcarbamoyl)-2-[2-(4-methoxyphenoxy)acetamido]-4-methylthiophene-3-carboxylate
0.01915
-
 pH 7.5, 37°C Brucella abortus (2E)-3-(2,3-dimethoxyphenyl)-N-[4-methyl-2-(4-methylpiperazin-1-yl)quinolin-6-yl]prop-2-enamide
0.02564
-
 pH 7.5, 37°C Brucella abortus 2-(4-ethoxyphenyl)-N-[3-(piperidin-1-yl)propyl]imidazo[2,1-b][1,3]benzothiazole-7-carboxamide
0.02638
-
 pH 7.5, 37°C Brucella abortus N-[3-(azepan-1-yl)propyl]-2-(4-methoxyphenyl)imidazo[2,1-b][1,3]benzothiazole-7-carboxamide
0.0278
-
 pH 7.5, 37°C Brucella abortus N-[3-(diethylamino)propyl]-2-(4-ethoxyphenyl)imidazo[2,1-b][1,3]benzothiazole-7-carboxamide
0.02964
-
 pH 7.5, 37°C Brucella abortus (2-ethyl-5-oxo-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7-yl)methyl 3,4,5-triethoxybenzoate
0.03053
-
 pH 7.5, 37°C Brucella abortus 5-[3-(propan-2-yl)-1H-pyrazol-5-yl]-3-(3,4,5-trimethoxyphenyl)-1,2,4-oxadiazole
0.03118
-
 pH 7.5, 37°C Brucella abortus 2-(4-methoxyphenyl)-N-[3-(piperidin-1-yl)propyl]imidazo[2,1-b][1,3]benzothiazole-7-carboxamide
0.03187
-
 pH 7.5, 37°C Brucella abortus N-[3-(diethylamino)propyl]-2-(4-methylphenyl)imidazo[2,1-b][1,3]benzothiazole-7-carboxamide

General Information

General Information Comment Organism
drug target the enzyme from Brucella abortus constitutes a suitable target for alternative antibacterial therapy, notably against strains resistant to conventional antibiotic treatments. A high-throughput screening for inhibitors of riboflavin synthase identifies antimicrobial compounds to treat brucellosis Brucella abortus