Synthesis and biological evaluation of new 1,2-dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for treatment of autoimmune disorders: structure-activity relationship.
نویسندگان
چکیده
Roquinimex-related 3-quinolinecarboxamide derivatives were prepared and evaluated for treatment of autoimmune disorders. The compounds were tested in mice for their inhibitory effects on disease development in the acute experimental autoimmune encephalomyelitis model and selected compounds in the beagle dog for induction of proinflammatory reaction. Structure-activity relationships are discussed. 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).
منابع مشابه
Green and efficient synthesis of trialkyl (E)-3-(3-Oxo-2-3,4-dihydro-2-(1H)-quinoxalinylidene)-prop-1-ene-1,2,3- tricarboxylates using K2CO3-PEG-400 as robust catalytic system
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ورودعنوان ژورنال:
- Journal of medicinal chemistry
دوره 47 8 شماره
صفحات -
تاریخ انتشار 2004