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Literature summary for 1.1.1.21 extracted from

  • Salem, M.G.; Abdel Aziz, Y.M.; Elewa, M.; Elshihawy, H.A.; Said, M.M.
    Molecular modelling and synthesis of spiroimidazolidine-2,4-diones with dual activities as hypoglycemic agents and selective inhibitors of aldose reductase (2018), Bioorg. Chem., 79, 131-144 .
    View publication on PubMed
Search for more literature for 1.1.1.21

Crystallization (Commentary)

Crystallization (Comment) Organism
molecular docking of inhibitors Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1'-(4-fluorobenzene-1-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione no selectivity for ALR2 over ALR1 Homo sapiens
1'-(5-chlorothiophene-2-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione 3.4fold selectivity for ALR2 over ALR1 Homo sapiens
1-(4-fluorophenyl)-1,3-diazaspiro[4.5]decane-2,4-dione 2.1fold selectivity for ALR2 over ALR1 Homo sapiens
1-(4-methoxyphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione 8.5fold selectivity for ALR2 over ALR1 Homo sapiens
1-(4-methylphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione 1.5fold selectivity for ALR2 over ALR1 Homo sapiens
1-(5-chlorothiophen-2-yl)-1,3-diazaspiro[4.5]decane-2,4-dione 1.9fold selectivity for ALR2 over ALR1 Homo sapiens
3'-(4-fluorobenzene-1-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione 10fold selectivity for ALR2 over ALR1 Homo sapiens
3'-(5-chlorothiophene-2-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione 1.1fold selectivity for ALR2 over ALR1 Homo sapiens
3-(4-fluorophenyl)-1,3-diazaspiro[4.5]decane-2,4-dione 2.3fold selectivity for ALR2 over ALR1 Homo sapiens
3-(4-methoxyphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione 1.2fold selectivity for ALR2 over ALR1 Homo sapiens
3-(4-methylphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione 11fold selectivity for ALR2 over ALR1 Homo sapiens
3-(5-chlorothiophen-2-yl)-1,3-diazaspiro[4.5]decane-2,4-dione 127fold selectivity for ALR2 over ALR1, 79% reduction in blood glucose level Homo sapiens
additional information synthesis of spiroimidazolidine-2,4-dione derivatives which preserve the minimum requirements of the proposed pharmacophoric models to enhance both activities. All compounds (except 1-(4-methoxyphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione) reduce the blood glucose level and all inhibit aldose reductase activity Homo sapiens
sorbinil
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P15121
-
-

Synonyms

Synonyms Comment Organism
AKR1B1
-
 Homo sapiens
ALR2
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00047
-
 pH 6.2, 33°C Homo sapiens 3-(5-chlorothiophen-2-yl)-1,3-diazaspiro[4.5]decane-2,4-dione
0.00162
-
 pH 6.2, 33°C Homo sapiens 3'-(4-fluorobenzene-1-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
0.00253
-
 pH 6.2, 33°C Homo sapiens 1-(4-methoxyphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
0.00353
-
 pH 6.2, 33°C Homo sapiens 3-(4-methylphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
0.00375
-
 pH 6.2, 33°C Homo sapiens 1'-(5-chlorothiophene-2-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
0.00478
-
 pH 6.2, 33°C Homo sapiens 1-(5-chlorothiophen-2-yl)-1,3-diazaspiro[4.5]decane-2,4-dione
0.00491
-
 pH 6.2, 33°C Homo sapiens 3'-(5-chlorothiophene-2-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
0.00768
-
 pH 6.2, 33°C Homo sapiens 3-(4-fluorophenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
0.00776
-
 pH 6.2, 33°C Homo sapiens 1-(4-fluorophenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
0.00831
-
 pH 6.2, 33°C Homo sapiens 3-(4-methoxyphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
0.00872
-
 pH 6.2, 33°C Homo sapiens 1-(4-methylphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
0.0111
-
 pH 6.2, 33°C Homo sapiens 1'-(4-fluorobenzene-1-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione