130421-48-6Relevant articles and documents
Pyrazole derivatives as potent inhibitors of c-Jun N-terminal kinase: Synthesis and SAR studies
Doma, Anuradha,Kulkarni, Ravindra,Palakodety, Radhakrishna,Sastry, G. Narahari,Sridhara, Janardhan,Garlapati, Achaiah
, p. 6209 - 6219 (2014/12/11)
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 9c, 10a and 10d were found to be potent among all the compounds.
