•Nitrogen heterocycles as new anti-Alzheimer's (AD) agents highlighting past molecular designs.•The development of safe, low-cost and highly active therapeutic agents incorporating nitrogen-containing heterocycles against AD is an important research topic.•Success stories of nitrogen-containing heterocyclic compounds in AD drug discovery.•We propose strategies for designing and developing novel potent anti-AD small molecules that can be used as treatments for AD. Alzheimer’s disease (AD) is a detrimental neurodegenerative disease that progressively worsens with time. Clinical options are limited and only provide symptomatic relief to AD patients. The search for effective anti-AD compounds is ongoing with a few already in Phase III clinical trials, yet to be approved. Heterocycles containing nitrogen are important to biological processes owing to their abundance in nature, their function as subunits of biological molecules and/or macromolecular structures, and their biological activities. The present review discusses previously used strategies, SAR, relevant in vitro and in vivo studies, and success stories of nitrogen-containing heterocyclic compounds in AD drug discovery. Also, we propose strategies for designing and developing novel potent anti-AD small molecules that can be used as treatments for AD.