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Synthesis and biological evaluation of new 1,2-dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for treatment of autoimmune disorders: structure-activity relationship.
- S. Jönsson, G. Andersson, +10 authors A. Björk
- Medicine, Chemistry
- Journal of medicinal chemistry
- 16 March 2004
Compound 8c, laquinimod, showed improved potency and superior toxicological profile compared to the lead compound roquinimex (1b, Linomide) and was selected for clinical studies (currently in phase II). Expand
The inhibitory effect in experimental autoimmune encephalomyelitis by the immunomodulatory drug Linomide (PNU-212616) is not mediated via release of endogenous glucocorticoids.
Results strongly suggest that Linomide does not exert its immunomodulatory activity via the release of endogenous glucocorticoids via the stimulation of the hypothalamic-pituitary-adrenal axis. Expand