当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis, structure-activity relationships, and pharmacokinetic properties of dihydroorotate dehydrogenase inhibitors: 2-cyano-3-cyclopropyl-3-hydroxy-N-[3'-methyl-4'-(trifluoromethyl)phenyl ] propenamide and related compounds.

Synthesis, structure-activity relationships, and pharmacokinetic properties of dihydroorotate dehydrogenase inhibitors: 2-cyano-3-cyclopropyl-3-hydroxy-N-[3'-methyl-4'-(trifluoromethyl)phenyl ] propenamide and related compounds.

Abstract：

:The active metabolite (2) of the novel immunosuppressive agent leflunomide (1) has been shown to inhibit the enzyme dihydroorotate dehydrogenase (DHODH). This enzyme catalyzes the fourth step in de novo pyrimidine biosynthesis. A series of analogues of the active metabolite 2 have been synthesized. Their in vivo biological activity determined in rat and mouse delayed type hypersensitivity has been found to correlate well with their in vitro DHODH potency. The most promising compound (3) has shown activity in rat and mouse collagen (II)-induced arthritis models (ED50 = 2 and 31 mg/kg, respectively) and has shown a shorter half-life in man when compared with leflunomide. Clinical studies in rheumatoid arthritis are in progress.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Kuo EA,Hambleton PT,Kay DP,Evans PL,Matharu SS,Little E,McDowall N,Jones CB,Hedgecock CJ,Yea CM,Chan AW,Hairsine PW,Ager IR,Tully WR,Williamson RA,Westwood R

doi

10.1021/jm9604437

subject

Has Abstract

pub_date

1996-11-08 00:00:00

pages

4608-21

issue

23

eissn

0022-2623

issn

1520-4804

pii

jm9604437

journal_volume

39

pub_type

杂志文章

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