Abstract
A facile synthesis of potential acetylcholinesterase (AChE) inhibitors, the tacrine analogues 3a-p, has been accomplished by direct cyclocondensation of 1-aryl-4-cyano-5-aminopyrazole with β-ketoesters using tin(IV) chloride as catalyst. The structures of all the compounds have been confirmed by IR, 1H- and 13C-NMR.
Highlights
Alzheimer’s disease (AD), the most common form of dementia among the elderly, is a progressive, degenerative disorder of the brain with a loss of memory and cognition [1]
Tacrine is a reversible inhibitor of acetylcholinesterase (AChE) that was launched in 1993 as the first drug for the treatment of AD [2]
The evaluation of the clinical effects of tacrine has shown efficacy in delaying the deterioration of the symptoms of AD, but the poor selectivity of this drug for AChE has resulted in a number of side effects, specially hepatotoxicity [3], and current research is focused on developing new
Summary
Alzheimer’s disease (AD), the most common form of dementia among the elderly, is a progressive, degenerative disorder of the brain with a loss of memory and cognition [1]. The evaluation of the clinical effects of tacrine has shown efficacy in delaying the deterioration of the symptoms of AD, but the poor selectivity of this drug for AChE has resulted in a number of side effects, specially hepatotoxicity [3], and current research is focused on developing new AChE inhibitors with improved activity and reduced adverse side effects, novel tacrine analogues have been reported [4,5,6,7,8,9,10,11,12,13,14,15,16,17,18]. Friedlander annulation is one of the simplest and most straightforward protocols for the preparation of quinoline derivatives [19,20]. It has been known for more than a century, it is still a hotspot of research. Molecules 2011, 16 aminopyrazole with β-ketoesters using SnCl4 as catalyst afforded the novel tacrine analogues 3a-p in good yields
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