Quinoline analogs are an important class of N-based heterocyclic compounds, which have received extensive attention because of their use in medicinal chemistry and organic synthesis. Over the past few decades, several new scaffold-based functionalization synthesis strategies have been reported for quinolines. Quinoline derivatives have a wide range of biological activities, includ-ing anti-Alzheimer''s disease activity. Herein, we review research on quinoline and related analogs as anti-Alzheimer''s disease agents from 2001 to 2022 and particularly highlight the structure-activity relationships and molecular binding modes. This review provides information for the rational design of more effective and target-specific drugs for Alzheimer''s disease.(c) 2022 The Author(s). Published by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).