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  • Title: Pyrazole derivatives as potent inhibitors of c-Jun N-terminal kinase: synthesis and SAR studies.
    Author: Doma A, Kulkarni R, Palakodety R, Sastry GN, Sridhara J, Garlapati A.
    Journal: Bioorg Med Chem; 2014 Nov 01; 22(21):6209-19. PubMed ID: 25261929.
    Abstract:
    Mitogen activated protein kinases including c-Jun N-terminal kinase play an indispensable role in inflammatory diseases. Investigation of reported JNK-1 inhibitors indicated that diverse heterocyclic compounds bearing an amide group rendered potent JNK-1 inhibitory activity which prompted us to synthesize new JNK-1 inhibitors containing a pyrazole heterocyclic group. A DABCO mediated 1,3-dipolar cycloaddition reaction in neat resulted in pyrazole carboxylic acid which was converted to desired amides. Upon confirmation of the structures, all the compounds were screened for JNK-1 inhibitory activity and in vivo anti-inflammatory activity. Several synthesized analogues have exhibited JNK-1 inhibitory activity less than 10 μM, in particular compounds 9 c, 10 a and 10 d were found to be potent among all the compounds.
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