SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors.

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Leban J, Kralik M, Mies J, Gassen M, Tentschert K, Baumgartner R

SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors.

Bioorg Med Chem Lett. 2005 Nov 1;15(21):4854-7.

PubMed ID

16143532 [ View in PubMed

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Abstract

Novel DHODH inhibitors were developed based on a previously described series by introduction of heteroatoms into the cyclopentene ring and hydroxyl groups attached to it. Also, the hydrophobic biphenyl side chain was replaced with benzyloxy phenyl groups. Activities on human, rat, and mouse enzymes indicate a species specificity of these inhibitors.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
2-({[3,5-DIFLUORO-3'-(TRIFLUOROMETHOXY)BIPHENYL-4-YL]AMINO}CARBONYL)CYCLOPENT-1-ENE-1-CARBOXYLIC ACID	Dihydroorotate dehydrogenase (quinone), mitochondrial	IC 50 (nM)	33	N/A	N/A	Details