Recent Advances In Tacrine-Based Anti-Alzheimer’s Drug Design

Alzheimer’s has become a common disease in aged people that leads to cognitive impairment and finally results in dementia and death. As the disease has a complicated etiology, it can hardly be prevented and cured. Hence, it turned out to be one of the menacing neurodegenerative diseases. The important concerning factor about Alzheimer’s is its unaffordable treatment cost. Also, there are only a few efficient anti-Alzheimer drugs. Now, it is a very urgent need to discover the most efficient and cost-effective anti-Alzheimer’s drugs. Nowadays, research reveals drugs based on heterocyclic scaffolds that have attributed to potent pharmacology. Quinoline-containing molecule, tacrine was recommended as an acetylcholinesterase inhibitor. However, its use has been withdrawn because of its toxicity. While research is going on designing derivatives of tacrine. Fortunately, some tacrine derivatives showed the most potent anti-Alzheimer properties. In view of this, here, anti-Alzheimer properties of recently reported tacrine-based Alzheimer’s agents are discussed and evaluated. The structure-activity relationship has been helpful in identifying potent molecules in a series of derivatives.

Keywords: Aβ-aggregation inhibitors, Anti-Alzheimer agents, Cholinesterase inhibitors, MAOs, Structure-activity relationship, Tacrine derivatives.