Dementia is a prevalent disease with estimated 36 million people currently affected. The most common disease 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 agonists have demonstrated excellent pro-cognitive profile in various animal models. In addition, 5-HT4 receptor agonists shift the equilibrium of APP processing from amyloidogenic to non-amyloidogenic pathway by activating alpha secretase enzyme.A new series of heteroaryl amide compounds was designed. The synthesized compounds are potent and selective 5-HT4 receptor agonists. A poster covering these aspects along with SAR, ADME and in vivo profiling (both in animal models of cognition and neurochemistry) will be presented.

Design and synthesis of newer amide derivatives as 5-HT<sub>4</sub> receptor ligands

248th National Meeting (2014)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.

Design and synthesis of newer amide derivatives as 5-HT4 receptor ligands

Design and synthesis of newer amide derivatives as 5-HT₄ receptor ligands