Synthesis & Biological Evaluation of Novel a - Methylarylacetic Acid Deriv Atives

Synthesis and biological evaluation of novel -methyl- arylacetic acid derivativesRheumatic diseases such as osteoarthritis and rheumatoid arthritis are the most prevalent causes of disability in humans. Inflammation, pain, joint destruction and deformity and impaired locomotor function are the common symptoms of these diseases. Nonsteroidal anti-inlflammatory drugs (NSAIDs) are among the most widely used therapeutics, primarily for the treatment of pain and inflammation. In the 1970s, a scientific breakthrough occurred with the elucidation of the molecular mechanism of aspirin and other NSAIDs. It had been shown that these anti-inflammatory substances block the biosynthesis of prostaglandins (PGs) which contribute to a variety of physiological and pathophysiological functions. PGs are biosynthesized from arachidonic acid under the catalytic action of cyclooxygenase (COX), which exists as two isoforms: COX-1 which catalyzes the production of cytoprotective PGs especially in the GIT and COX-2 which mediates inflammation. The traditional NSAIDS non-selectively inhibit both isoforms of COX and therefore have anti-inflammatory effect but with harmful effects on the GIT especially on long-term use. The discovery of a second isoform of COX had t