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Literature summary for 1.14.14.25 extracted from

  • Uto, Y.
    Imidazo[1,2-a]pyridines as cholesterol 24-hydroxylase (CYP46A1) inhibitors: a patent evaluation (WO2014061676) (2015), Expert Opin. Ther. Pat., 25, 373-377.
    View publication on PubMed

Application

Application Comment Organism
drug development generation of imidazo[1,2-a]pyridine analogues that effectively inhibit cholesterol 24-hydroxylase (CYP46A1). They can be used for prophylactic treatment of neurodegenerative disorders, such as Alzheimer's disease and Parkinson's disease Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)[8-(1,3-oxazol-5-yl)-6-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl]methanone
-
Homo sapiens
(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)[8-(1,3-oxazol-5-yl)-6-(trifluoromethyl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]methanone
-
Homo sapiens
(4-benzyl-4-hydroxypiperidin-1-yl)([2,4'-bipyridin]-3-yl)methanone
-
Homo sapiens
1-[3-(3-oxa-8-azabicyclo[3.2.1]octane-8-carbonyl)-6-(trifluoromethyl)imidazo[1,2-a]pyridin-8-yl]-4H-1,2,4-triazol-1-ium
-
Homo sapiens
2-[5-methyl-1-(pyridine-4-carbonyl)-5-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-3-yl]benzonitrile
-
Homo sapiens
8-(1,3-oxazol-5-yl)-N-phenyl-6-(trifluoromethyl)imidazo[1,2-a]pyridine-3-carboxamide
-
Homo sapiens
additional information generation of a series of imidazo[1,2-a]pyridine analogues that effectively inhibit cholesterol 24-hydroxylase (CYP46A1), synthesis and evaluation, overview Homo sapiens
N-benzyl-8-(1,3-oxazol-5-yl)-6-(trifluoromethyl)imidazo[1,2-a]pyridine-3-carboxamide
-
Homo sapiens
voriconazole
-
Homo sapiens
[6-cyclopropyl-8-(1,3-oxazol-5-yl)imidazo[1,2-a]pyridin-3-yl](3-oxa-8-azabicyclo[3.2.1]octan-8-yl)methanone
-
Homo sapiens
[6-fluoro-8-(1,3-oxazol-5-yl)imidazo[1,2-a]pyridin-3-yl](3-oxa-8-azabicyclo[3.2.1]octan-8-yl)methanone
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cholesterol + [reduced NADPH-hemoprotein reductase] + O2 Homo sapiens
-
(24S)-cholest-5-ene-3beta,24-diol + [oxidized NADPH-hemoprotein reductase] + H2O
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y6A2 gene CYP46A1
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cholesterol + [reduced NADPH-hemoprotein reductase] + O2
-
Homo sapiens (24S)-cholest-5-ene-3beta,24-diol + [oxidized NADPH-hemoprotein reductase] + H2O
-
?

Synonyms

Synonyms Comment Organism
CYP46A1
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

General Information

General Information Comment Organism
malfunction polymorphisms in the CYP46 gene and CYP46A1 enzyme dysfunction are involved in neurodegenerative disorders, such as Alzheimer's disease and Parkinson's disease. The 24(S)-hydroxycholesterol levels in cerebrospinal fluid are higher in patients with Alzheimer's disease compared to healthy control. CYP46A1 inhibition by voriconazole decreases 24S-hydroxycholesterol levels in the retina and affects cholesterol homeostasis and function in the retina Homo sapiens