title: SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors.
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.
authors.affiliation: 4SC AG, Am Klopferspitz 19a, 82152 Martinsried, Germany. leban@4sc.com
authors.forename: Johann
authors.initials: J
authors.lastname: Leban
authors.forename: Martin
authors.initials: M
authors.lastname: Kralik
authors.forename: Jan
authors.initials: J
authors.lastname: Mies
authors.forename: Michael
authors.initials: M
authors.lastname: Gassen
authors.forename: Karin
authors.initials: K
authors.lastname: Tentschert
authors.forename: Roland
authors.initials: R
authors.lastname: Baumgartner
mesh_terms: D000577:Amides; D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects*; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000494:pharmacology; D004081:Dihydroorotate Oxidase / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007166:Immunosuppressive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007963:Leukocytes, Mononuclear / Q000166:cytology / Q000187:drug effects; D051379:Mice; D051381:Rats; D013045:Species Specificity; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D003517:Cyclopentanes; D004791:Enzyme Inhibitors; D007166:Immunosuppressive Agents; C409963:cyclopentenedicarboxylic acid; D004081:Dihydroorotate Oxidase