Inflammation is the first response of the immune system to harmful stimuli such as infection or irritation, consists of a cascade of biochemical events that propagates and matures the inflammatory response. Number of anti-inflammatory drugs are available for treatment of acute and chronic inflammation. Many anti-inflammatory drugs cause adverse side effects. The quinoline class of compounds are important for searching the safe and effective anti-inflammatory drugs. These drugs are classified based on the number of substituents present on the quinoline ring or compounds containing a quinoline ring fused to other heterocyclic compounds. Quinolines have the ability to target several causes of inflammation includes transient receptor potential vanilloid 1 receptor. The TRPV1 receptor, first cloned and characterized in 1997, is a non-selective cation channel expressed in primary sensory neurons, and is a key pain sensor and integrator. This review provides the discovery of various quinoline derivatives as transient receptor potential vanilloid 1 (TRPV1) antagonists. Overall, the quinoline moiety will be used as a new template for designing and identifying the novel anti-inflammatory drugs in future.
 Keywords: Quinoline, Inflammation, Transient receptor Potential Vanilloid 1, Antagonists.