Pyrazole derivatives as potent inhibitors of c-Jun N-terminal kinase: Synthesis and SAR studies
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.
Doma, Anuradha,Kulkarni, Ravindra,Palakodety, Radhakrishna,Sastry, G. Narahari,Sridhara, Janardhan,Garlapati, Achaiah
p. 6209 - 6219
(2014/12/11)
SYNTHESIS AND BIOLOGICAL ACTIVITY OF HETERYLAMIDES OF AROYLPYRUVIC ACIDS AND 5-ARYLPYRAZOLE-3-CARBOXYLIC ACIDS
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Andreichikov, Yu. S.,Milyutin, A. V.,Krylova, I. V.,Saraeva, R. F.,Dormidontova, E. V.,et al.
p. 473 - 476
(2007/10/02)
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