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Heterocyclic systems with a quinoline nucleus represent privileged moieties in medicinal chemistry and drug discovery due to the broad biological activities displayed by this scaffold. Among others, quinolines have shown antimalarial, anticancer, antitubercular, antiviral, antibiotic, antileishmanial, and cardiovascular properties. Due to the versatility of the quinoline skeleton, it has attracted the attention of both medicinal and organic chemists for decades, which has prompted the development of several synthetic methods towards this moiety. In this chapter, the synthesis and pharmacological properties of this scaffold will be summarized.

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