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 (2014) Pyrazole derivatives as potent inhibitors of c-Jun N-terminal kinase: synthesis and SAR studies Bioorganic & Medicinal Chemistry, 22 (21). pp. 6209-6219. ISSN 0968-0896

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Official URL: http://www.sciencedirect.com/science/article/pii/S...

Related URL: http://dx.doi.org/10.1016/j.bmc.2014.08.028

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 9c, 10a and 10d were found to be potent among all the compounds.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:JNK-1; Inflammation; Pyrazoles; IC50
ID Code:108637
Deposited On:27 Jul 2017 12:37
Last Modified:27 Jul 2017 12:38

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