The identification of various enzymes participating in the arachidonic acid metabolism and recognition of inflammatory metabolites led to systematic studies for the development of anti-inflammatory drugs. Starting with the stimulatory role of phospholipases to release arachidonic acid from phospholipids, over-expression of cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) enzymes cause more than normal production of the respective metabolites. Excessive production of prostaglandins and leukotrienes leads to the manifestation of acute to chronic inflammation in humans. The consequent ailments are expressed in the form of asthma, atherosclerosis, irritable bowel syndrome, arthritis and cancer. Targeting the induced isoform of cyclooxygenase viz. cyclooxygenase-2 (COX-2) and 5-LOX enzyme has opened new aspects for capping the enzyme mediated inflammation. A number of such aspects have been discussed in this comprehensive review.