Synthesis of a new analogue of anti-alzheimer drug tacrine
Alzheimer’s disease (AD) is a severe age-dependent neurodegenerative brain disorder associated with progressive memory loss and decrease of cognitive functions. The absence of a cure so far and the expected dramatic incidence increase in the coming years, due to the population aging, place a huge burden on society, which has accounted for the current intensive studies aimed at preventing and treating AD. Tacrine (trade name Cognex®), the first clinically effective acetylcholinesterase inhibitor, was approved for the treatment of mild to moderate AD. Unfortunately, frequent adverse effects including peripheral cholinergic effects and hepatotoxicity limited its therapeutic potential. However, its high potency in cholinesterase inhibition, low molecular weight, and simple structure make tacrine a promising scaffold for developing new multi-target agents. In this work, we started our investigation on the development of sulfur-containing tacrine analogues.