4.7 Review

Pivotal role of nitrogen heterocycles in Alzheimer's disease drug discovery

Journal

DRUG DISCOVERY TODAY
Volume 27, Issue 10, Pages -

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2022.07.007

Keywords

Alzheimer's disease; Drug discovery; Multi-target directed ligands; Nitrogen heterocycles

Funding

  1. Department of Defense [W81XWH210053]

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Alzheimer's disease is a progressive neurodegenerative disease with limited clinical options. Research is ongoing to find effective anti-AD compounds, and this review explores previous strategies, research findings, and success stories. Strategies for designing and developing small molecules for AD treatment are also proposed.
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.

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