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Quinolinone is a heterocyclic aromatic organic compound. Quinolinone derivatives are having very much usefulness in current therapeutic applications in medicinal chemistry and pharmacology. This compounds having the bicyclic in nature having the fusion of benzene and pyridine the basic moiety present in quinolinones. It is an important pharmacophore and privileged structure in medicinal chemistry. Chromenoquinolinones, isoquinolinones and 4-quinolinones plays a very important role with plenty of useful therapeutic activities such as: antiulcers, antihypertensives, analgesic, anti-inflammatory, anti-virals, antifungals, anticancers, and antihistaminics. The review of the literature shows that the quinolinones derivatives are outstandingly effective compound and number of reviews available for biochemical and pharmacological studies conformed that their molecules are useful against a wide variety of micro-organisms. Because of their importance, the methods for their synthesis have become a focus of synthetic organic chemists. Therefore in the present review we tried to compile the chemistry of different derivative of substituted quinolinones as well as various pharmacological activities and some of the important methodologies used for the synthesis.