Biphenyl-4-ylcarbamoyl thiophene carboxylic acids as potent DHODH inhibitors.

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Leban J, Kralik M, Mies J, Baumgartner R, Gassen M, Tasler S

Biphenyl-4-ylcarbamoyl thiophene carboxylic acids as potent DHODH inhibitors.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):267-70. Epub 2005 Oct 21.

PubMed ID

16246558 [ View in PubMed

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Abstract

A previously discovered DHODH inhibitor series was further improved by replacing the cyclopentene ring by aromatic heterocycles. Different isomers of these compounds were prepared by the directed ortho-metallation procedure. The compounds are more active than the corresponding cyclopentene analogs and show potent effects on PBMC's proliferation.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
3-{[(3-FLUORO-3'-METHOXYBIPHENYL-4-YL)AMINO]CARBONYL}THIOPHENE-2-CARBOXYLIC ACID	Dihydroorotate dehydrogenase (quinone), mitochondrial	IC 50 (nM)	44	8	25	Details
Brequinar	Dihydroorotate dehydrogenase (quinone), mitochondrial	IC 50 (nM)	8	8	25	Details