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 |
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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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