Literature summary for 1.14.19.30 extracted from

Fujimoto, J.; Okamoto, R.; Noguchi, N.; Hara, R.; Masada, S.; Kawamoto, T.; Nagase, H.; Tamura, Y.O.; Imanishi, M.; Takagahara, S.; Kubo, K.; Tohyama, K.; Iida, K.; Andou, T.; Miyahisa, I.; Matsui, J.; Hayashi, R.; Maekawa, T.; Matsunaga, N.
Discovery of 3,5-diphenyl-4-methyl-1,3-oxazolidin-2-ones as novel, potent, and orally available DELTA-5 desaturase (D5D) inhibitors (2017), J. Med. Chem., 60, 8963-8981 .

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Application

Application	Comment	Organism
medicine	Delta5 desaturase inhibitors are expected to drive anti-inflammatory properties through reduction of arachidonic acid biosynthesis and simultaneous accumulation of dihomo-gamma-linolenic acid	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
3,5-diphenyl-1,3-oxazolidin-2-one	-	Homo sapiens
3,5-diphenyl-1,3-oxazolidin-2-one	-	Mus musculus
3,5-diphenyl-1,3-oxazolidin-2-one	-	Rattus norvegicus
3-[(4S,5S)-5-(4-fluorophenyl)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]benzonitrile	derivative with improved metabolic stability	Homo sapiens
3-[(4S,5S)-5-(4-fluorophenyl)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]benzonitrile	derivative with improved metabolic stability	Mus musculus
3-[(4S,5S)-5-(4-fluorophenyl)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]benzonitrile	derivative with improved metabolic stability	Rattus norvegicus
5-[(4S,5S)-5-(4-fluorophenyl)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]benzene-1,3-dicarbonitrile	-	Homo sapiens
5-[(4S,5S)-5-(4-fluorophenyl)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]benzene-1,3-dicarbonitrile	inhibitor endowed with excellent DELTA5 desaturase binding affinity, cellular activity, and high oral bioavailability in a mouse. It exhibits robust in vivo hepatic arachidonic acid/dihomo-gamma-linolenic acid ratio reduction (a target engagement marker) in an atherosclerosis mouse model	Mus musculus
5-[(4S,5S)-5-(4-fluorophenyl)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]benzene-1,3-dicarbonitrile	-	Rattus norvegicus

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
microsome	-	Rattus norvegicus	-	-
microsome	-	Mus musculus	-	-
microsome	-	Homo sapiens	-	-

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	O60427	-	-
Mus musculus	Q920L1	-	-
Rattus norvegicus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
liver	-	Rattus norvegicus	-
liver	-	Mus musculus	-
liver	-	Homo sapiens	-

Synonyms

Synonyms	Comment	Organism
D5D	-	Rattus norvegicus
D5D	-	Mus musculus
D5D	-	Homo sapiens
DELTA5 desaturase	-	Rattus norvegicus
DELTA5 desaturase	-	Mus musculus
DELTA5 desaturase	-	Homo sapiens

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Release 2023.1 (January 2023)