Pyrazolones as therapeutics for kinase-mediated inflammatory disorders

Abstract

Many of the current approaches toward therapies for inflammatory diseases target the inhibition of various kinases. Overexpression or inappropriate activation of these kinases is known to trigger various inflammatory diseases via aberrant phosphorylation of protein targets, including inflammatory diseases such as rheumatoid arthritis (RA), osteoarthritis (OA) and inflammatory bowel disease (IBD). A series of pyrazolone-based kinase inhibitors are presented with some biological data for a few of the representative compounds. These publications demonstrate the versatility of the pyrazolone heterocycle as an ATP mimetic.

Keywords::

• arthritis
• ATP mimetic
• bicyclic pyrazolone
• inflammation
• kinase
• p38 mitogen-activated protein kinase (MAPK)
• pyrazolone