Abstract: Alzheimer's disease (AD), a prevalent neurodegenerative disorder, significantly impairs patients' cognitive functions and quality of life, with no definitive cure currently available. Consequently, there is an urgent necessity to explore and develop promising novel drug molecules. Quinoline and isoquinoline derivatives have emerged as key candidates in AD research owing to their diverse pharmacological activities, particularly in inhibiting the aggregation of amyloid β-protein (Aβ), reducing the phosphorylation of tubulin-associated unit (Tau) proteins, modulating the cholinergic system, and exhibiting anti-inflammatory and antioxidant properties. This article provides an overview of the latest advancements in the study of quinoline and isoquinoline derivatives for AD, emphasizing their performance in both in vitro and in vivo biological evaluations. It further elucidates their mechanisms of action in combating Aβ accumulation, regulating Tau dephosphorylation, ameliorating cholinergic system imbalances, and suppressing neuroinflammatory responses, serving as a reference for further research into the application of quinoline and isoquinoline derivatives in AD treatment.