Dementia is a prevalent disease with estimated 36 million people currently affected. The most common group representing such patient pool is Alzheimer's disease (AD). AD is a progressive neurodegenerative disorder with ageing as the major risk factor. Extracellular beta amyloid deposits and intracellular tau tangles in brain provide the best differentiator of AD from other forms of dementia. Current therapies treat only the disease symptoms and are associated with modest efficacy, offset by dose-limiting side effects. 5-HT4 receptor partial agonist shift the equilibrium of APP processing from amyloidogenic to non-amyloidogenic pathway by activating alpha secretase enzyme and demonstrated excellent pro-cognitive profile in various animal models. Herein, we report our initial findings towards identification of a novel series of 5-HT4 receptor partial agonists. Compounds from this series have shown good selectivity, pharmacokinetic properties, adequate brain penetration and activity in animal models of cognition. Details will be presented in the poster.

Discovery of 5-HT4 receptor partial agonist for the treatment of Alzheimer's disease

243rd National Meeting (2012)

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