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Literature summary for 1.1.1.21 extracted from

  • Celestina, S.; Sundaram, K.; Ravi, S.
    In vitro studies of potent aldose reductase inhibitors Synthesis, characterization, biological evaluation and docking analysis of rhodanine-3-hippuric acid derivatives (2020), Bioorg. Chem., 97, 103640 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(4-((E)-4-oxo-5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-4-oxo-5-((1-phenyl-3-m-tolyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-4-oxo-5-((1-phenyl-3-p-tolyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-5-((3-(3-bromophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-5-((3-(3-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-5-((3-(3-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-5-((3-(3-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-5-((3-(3-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-5-((3-(4-bromophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido) acetic acid
-
Rattus norvegicus
2-(4-((E)-5-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-5-((3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-5-((3-(4-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido)acetic acid
-
Rattus norvegicus
2-(4-((E)-5-((3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
Rattus norvegicus
additional information synthesis of derivatives of rhodanine-3-hippuric acid-pyrazole hybrid. All the compounds exhibit a well-defined binding mode within the aldose reductase active site, with the anion head group bound to the catalytic center, blocking thus its activity Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
ALR2
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00004
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-5-((3-(3-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
0.00006
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-4-oxo-5-((1-phenyl-3-m-tolyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
0.00008
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-5-((3-(3-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
0.00036
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-5-((3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
0.00064
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-4-oxo-5-((1-phenyl-3-p-tolyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
0.00076
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-5-((3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
0.00087
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-5-((3-(3-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
0.0009
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-5-((3-(3-bromophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
0.00098
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-5-((3-(3-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido)acetic acid
0.0011
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-5-((3-(4-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido)acetic acid
0.00112
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-5-((3-(4-bromophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido) acetic acid
0.00116
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-4-oxo-5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
0.00136
-
37°C, pH not specified in the publication Rattus norvegicus 2-(4-((E)-5-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid