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Literature summary extracted from

  • Studzinska, R.; Kupczyk, D.; Plazinska, A.; Kolodziejska, R.; Kosmalski, T.; Modzelewska-Banachiewicz, B.
    Thiazolo[3,2-a]pyrimidin-5-one derivatives as a novel class of 11beta-hydroxysteroid dehydrogenase inhibitors (2018), Bioorg. Chem., 81, 21-26 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.146 2,6,7-trimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 30.88% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2,6-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2,7-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 17.65% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2,7-dimethyl-6-nitro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2-(bromomethyl)-6,7-dimethyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 33.82% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2-(bromomethyl)-7-methyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 2.94% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2-(bromomethyl)-7-methyl-6-nitro-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 32.35% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2-(iodomethyl)-2,3,6,7,8,9-hexahydro-5H-[1,3]thiazolo[2,3-b]quinazolin-5-one 27.94% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2-(iodomethyl)-2,3,7,8,9,10-hexahydrocyclohepta[d][1,3]thiazolo[3,2-a]pyrimidin-5(6H)-one 23.53% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2-(iodomethyl)-6-methyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 13.24% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 29.41% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2-methyl-6,7,8,9-tetrahydro-5H-[1,3]thiazolo[2,3-b]quinazolin-5-one 13.24% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 2-methyl-7,8,9,10-tetrahydrocyclohepta[d][1,3]thiazolo[3,2-a]pyrimidin-5(6H)-one 14.71% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 6-bromo-2,7-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 2.94% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 6-bromo-2-(bromomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 25% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 6-bromo-2-(iodomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 32.35% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 7-(cyclohexylmethyl)-2-iodomethyl-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-one selective inhibitor for isoform 11beta-HSD1, 59.15% inhibition of isoform 11beta-HSD1 at 0.01 mM, 4.74% inhibition of isoform 11beta-HSD2 at 0.01 mM Homo sapiens
1.1.1.146 7-(cyclohexylmethyl)-2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 27.94% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 7-ethyl-2-(iodomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 7-ethyl-2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 23.53% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens
1.1.1.146 carbenoxolone 89.7% inhibition of isoform 11beta-HSD1 at 0.01 mM Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.146 microsome
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.146 cortisone + NADPH + H+ Homo sapiens
-
 cortisol + NADP+
-
 ir

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.146 Homo sapiens P28845
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.146 adipose tissue
-
 Homo sapiens
-
1.1.1.146 brain
-
 Homo sapiens
-
1.1.1.146 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.146 cortisone + NADPH + H+
-
 Homo sapiens cortisol + NADP+
-
 ir

Synonyms

EC Number Synonyms Comment Organism
1.1.1.146 11beta-HSD1 isoform Homo sapiens
1.1.1.146 11beta-hydroxysteroid dehydrogenase
-
 Homo sapiens
1.1.1.146 11beta-hydroxysteroid type 1 dehydrogenase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.146 NADPH dependent on Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.146 0.0069
-
 isoform 11beta-HSD1, at pH 7.4 and 37°C Homo sapiens 7-(cyclohexylmethyl)-2-iodomethyl-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-one