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The nature of inflammation and relationship with metabolism of unsaturated fatty acid, and the factors effect on it were shown in this book. The non-steroidal anti-inflammatory drugs (NSAIDs) have side effects and non specific even that specific for cyclooxygenase-2 (COX-2) enzyme, amino acids derivatives were synthesised and tested for anti-inflammatory and analgesic activity. The nature of binding of compounds with the active site of enzyme specify the activity of drugs, they appeared highly activity and high-quality for used as novel anti-inflammatory drugs, without side effects. The histidine derivatives show potent activity as a new anti-inflammatory and analgesic analogue, also tryptophan derivatives they more powerful than aspirin and diclofenac, they contain imidazole ring in their structure. The future of anti-inflammatory drugs (NSAIDs) is amino acids derivatives, and possibly works as anti-cancer drugs.