Abstract

SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF P38 KINASE INHIBITOR AS ANTIINFLAMMATORY AGENT

Mithilesh Singh* and Dr. Ashish Kumar Sharma

ABSTRACT

Inflammation occurs as a defensive process by the organism followed by redness, heat, swelling and pain due to damage to the tissues or the organs. With the help of this mechanism our body fight with the pathogens such as parasites, bacteria, virus and other harmful microorganisms. There are various disease caused by chronic inflammation including gastritis, colitis, dermatitis, rheumatoid arthritis, pulmonary diseases, and type II diabetes, which causes damage to millions of people’s health every year. There are so many growing evidences that show that inflammation is a critical initiation factor which induces a variety of other major diseases such as cancer, atherosclerosis, Alzheimer’s disease, cardiovascular disease, neurological disorders, and pulmonary diseases. Therefore knowing deeply about inflammation is basically required for better treatment strategies. P38 mitogen-activated protein kinases are a class of mitogen-activated protein kinases which are responsive to stress stimuli, such as cytokines, ultraviolet irradiation, heat shock, and osmotic shock, and are involved in cell differentiation and apoptosis. P38 MAP Kinase (MAPK), also called RK or CSBP, is the mammalian orthologue of the yeast HOG kinase which participates in a signalling cascade controlling cellular responses to cytokines and stress. Numerous p38 kinase inhibitors have been reported and some of them are various stage of clinical evaluation. New analogue containing α-ketoamides were synthesized and evaluate for p38 kinase inhibitory activity and reported to other then ATP binding site.

Keywords: MAPK, P38 KINASE Inhibitors, ATP Binding Site, ?-ketoamides.