期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 21, 页码 6209-6219出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.08.028
关键词
JNK-1; Inflammation; Pyrazoles; IC50
资金
- AICTE, India [8023/RID/BOR/MOD-111./2007-08]
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 mu M, in particular compounds 9c, 10a and 10d were found to be potent among all the compounds. (C) 2014 Elsevier Ltd. All rights reserved.
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