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Literature summary extracted from

  • Noureldin, N.A.; Kothayer, H.; Lashine, E.M.; Baraka, M.M.; Huang, Y.; Li, B.; Ji, Q.
    Design, synthesis and biological evaluation of novel quinazoline-2,4-diones conjugated with different amino acids as potential chitin synthase inhibitors (2018), Eur. J. Med. Chem., 152, 560-569 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.16 1-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetyl)pyrrolidine-2-carboxylic acid 75.5% inhibition at 0.3 mg/ml Saccharomyces cerevisiae
2.4.1.16 2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)-3-(4-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetoxy)phenyl)propanoic acid 65.3% inhibition at 0.3 mg/ml Saccharomyces cerevisiae
2.4.1.16 2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)-3-phenylpropanoic acid
-
 Saccharomyces cerevisiae
2.4.1.16 2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)-4-(methylthio)butanoic acid
-
 Saccharomyces cerevisiae
2.4.1.16 2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)acetic acid
-
 Saccharomyces cerevisiae
2.4.1.16 2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)butanoic acid
-
 Saccharomyces cerevisiae
2.4.1.16 2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid
-
 Saccharomyces cerevisiae
2.4.1.16 3-(1H-imidazol-5-yl)-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid 61.5% inhibition at 0.3 mg/ml Saccharomyces cerevisiae
2.4.1.16 3-(1H-indol-3-yl)-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid
-
 Saccharomyces cerevisiae
2.4.1.16 3-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid
-
 Saccharomyces cerevisiae
2.4.1.16 3-hydroxy-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid
-
 Saccharomyces cerevisiae
2.4.1.16 3-methyl-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)butanoic acid
-
 Saccharomyces cerevisiae
2.4.1.16 4-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)butanoic acid 68.2% inhibition at 0.3 mg/ml Saccharomyces cerevisiae
2.4.1.16 4-methyl-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)pentanoic acid
-
 Saccharomyces cerevisiae
2.4.1.16 5-[(3,6,6-trimethylhept-4-yn-1-yl)amino]quinolin-2(1H)-one
-
 Saccharomyces cerevisiae
2.4.1.16 5-[(6,6-dimethylhepta-2,4-diyn-1-yl)(methyl)amino]-3,4-dihydroquinolin-2(1H)-one
-
 Saccharomyces cerevisiae
2.4.1.16 8-[(6,6-dimethylhepta-2,4-diyn-1-yl)(methyl)amino]-2H-1,4-benzoxazin-3(4H)-one
-
 Saccharomyces cerevisiae
2.4.1.16 Polyoxin B
-
 Saccharomyces cerevisiae

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.1.16 UDP-N-acetyl-alpha-D-glucosamine + [(1->4)-N-acetyl-beta-D-glucosaminyl]n Saccharomyces cerevisiae
-
 UDP + [(1->4)-N-acetyl-beta-D-glucosaminyl]n+1
-
 ?
2.4.1.16 UDP-N-acetyl-alpha-D-glucosamine + [(1->4)-N-acetyl-beta-D-glucosaminyl]n Saccharomyces cerevisiae CGMCC2.145
-
 UDP + [(1->4)-N-acetyl-beta-D-glucosaminyl]n+1
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.16 Saccharomyces cerevisiae
-
-
-
2.4.1.16 Saccharomyces cerevisiae CGMCC2.145
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.16 UDP-N-acetyl-alpha-D-glucosamine + [(1->4)-N-acetyl-beta-D-glucosaminyl]n
-
 Saccharomyces cerevisiae UDP + [(1->4)-N-acetyl-beta-D-glucosaminyl]n+1
-
 ?
2.4.1.16 UDP-N-acetyl-alpha-D-glucosamine + [(1->4)-N-acetyl-beta-D-glucosaminyl]n
-
 Saccharomyces cerevisiae CGMCC2.145 UDP + [(1->4)-N-acetyl-beta-D-glucosaminyl]n+1
-
 ?
2.4.1.16 UDP-N-acetyl-D-glucosamine + N-acetyl-D-glucosamine
-
 Saccharomyces cerevisiae UDP + 1,4-(N-acetyl-beta-D-glucosaminyl)2
-
 ?
2.4.1.16 UDP-N-acetyl-D-glucosamine + N-acetyl-D-glucosamine
-
 Saccharomyces cerevisiae CGMCC2.145 UDP + 1,4-(N-acetyl-beta-D-glucosaminyl)2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.16 CHS
-
 Saccharomyces cerevisiae

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.16 0.166
-
 at pH 7.5 and 37°C Saccharomyces cerevisiae 2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)-3-(4-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetoxy)phenyl)propanoic acid
2.4.1.16 0.17
-
 at pH 7.5 and 37°C Saccharomyces cerevisiae Polyoxin B
2.4.1.16 0.18
-
 at pH 7.5 and 37°C Saccharomyces cerevisiae 1-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetyl)pyrrolidine-2-carboxylic acid
2.4.1.16 0.3
-
 at pH 7.5 and 37°C Saccharomyces cerevisiae 3-(1H-imidazol-5-yl)-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid
2.4.1.16 0.3
-
 at pH 7.5 and 37°C Saccharomyces cerevisiae 4-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)butanoic acid