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Literature summary for 1.1.1.21 extracted from

  • Pegklidou, K.; Koukoulitsa, C.; Nicolaou, I.; Demopoulos, V.J.
    Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisosterism between a carboxylic acid moiety and that of a tetrazole (2010), Bioorg. Med. Chem., 18, 2107-2114.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
((1-(2H-tetrazol-5-yl)methyl)-1H-pyrrol-3-yl)(phenyl)-methanone 40% inhibition Rattus norvegicus
(1-(2-(2H-tetrazol-5-yl)ethyl)-1H-pyrrol-3-yl)(phenyl)-methanone 6% inhibition Rattus norvegicus
(1-(2H-tetrazole-5-yl)-1H-pyrrol-2-yl)(phenyl)-methanone
-
Rattus norvegicus
(1-(2H-tetrazole-5-yl)-1H-pyrrol-3-yl)(phenyl)-methanone
-
Rattus norvegicus
(1-(3-(2H-tetrazol-5-yl)propyl)-1H-pyrrol-3-yl)(phenyl)-methanone 41% inhibition Rattus norvegicus
2-(3-benzoyl-1H-pyrrol-1-yl)acetic acid
-
Rattus norvegicus
3-(3-benzoyl-1H-pyrrol-1-yl)propanoic acid
-
Rattus norvegicus
4-(3-benzoyl-1H-pyrrol-1-yl)butanoic acid
-
Rattus norvegicus
additional information design and synthesis of pyrrole based inhibitors and evaluation as selective aldose reductase inhibitors, bioisosterism between a carboxylic acid moiety and that of a tetrazole, overview Rattus norvegicus
sorbinil
-
Rattus norvegicus
Valproic acid
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
ALR2 partially from lenses Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
lens ALR2 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-glucuronate + NADPH
-
Rattus norvegicus ?
-
?

Synonyms

Synonyms Comment Organism
aldose reductase
-
Rattus norvegicus
ALR2
-
Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.2
-
assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00025
-
pH 7.2, temperature not specified in the publication Rattus norvegicus sorbinil
0.002
-
pH 7.2, temperature not specified in the publication Rattus norvegicus 2-(3-benzoyl-1H-pyrrol-1-yl)acetic acid
0.006
-
pH 7.2, temperature not specified in the publication Rattus norvegicus 4-(3-benzoyl-1H-pyrrol-1-yl)butanoic acid
0.0097
-
pH 7.2, temperature not specified in the publication Rattus norvegicus 3-(3-benzoyl-1H-pyrrol-1-yl)propanoic acid
0.018
-
pH 7.2, temperature not specified in the publication Rattus norvegicus (1-(2H-tetrazole-5-yl)-1H-pyrrol-3-yl)(phenyl)-methanone
0.02
-
pH 7.2, temperature not specified in the publication Rattus norvegicus (1-(2H-tetrazole-5-yl)-1H-pyrrol-2-yl)(phenyl)-methanone
0.0501
-
pH 7.2, temperature not specified in the publication Rattus norvegicus Valproic acid