Alzheimer's disease (AD) is the most common form of dementia among older people, which initially affects the parts of the brain that control thought, memory and language. Therefore its first symptoms are: confusion, disturbances in short-term memory, personality changes and language difficulties. They are thought to be related to the degeneration of cholinergic neurons in the cerebral cortex and subcortical structures. Since putting forward this hypothesis, known today as the cholinergic theory, the substances which enhance the cholinergic transmission have been searched. Among possible strategies cholinesterase inhibitors are the only class of compounds to date, that have consistently proven to be efficacious in treating the cognitive and functional symptoms of AD. Four of these belonging to different chemical groups have been approved for the symptomatic treatment of mild to moderate AD: tacrine (aminoacridine), donepezil (benzylpiperidine), galantamine (a tertiary alkaloid) and rivastigmine (carbamate). However, none of these is efficient enough and consequently it is necessary to search for new ones [1, 2].

Our research group has managed to synthesize potential new inhibitors of cholinesterase. After analyzing the available data, considering especially the interactions between certain structures and active site of cholinesterase, we designed and obtained two series of compounds. Taking rivastigmine as a structural model, both series contain carbamoyl moiety attached directly to the phenyl ring, and one of them contains also benzylpiperidine fragment which is crucial for the activity of donepezil.

Both series will be tested with Ellman's method to examine their cholinesterase inhibition activity.

1. M. Bolognesi; J. Med. Chem., 2004, 47, 5945-52

2. M. Recanatini; Curr. Pharmac. Des., 2004, 10, 3157-66

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