A series of novel indolizine derivatives have been designed and synthesized which have shown potent partial agonist activity towards 5-HT4 receptors. The SAR was done to obtain the compounds which have favorable ADME properties and potent efficacy in animal models of cognition. These compounds can be used in treating cognition deficits associated with Alzheimer's disease (AD), which is the most prevalent type of dementia in the elderly and is characterized by the appearance of amyloid plaques (A�), synaptic loss and cholinergic hypofunction. Serotonin 5-HT4Rs are widely expressed throughout the body, but in all species studied so far, the highest density of 5-HT4R is observed in the CNS. Several literature evidences suggest a role of 5-HT4 agonist in cognition.

Novel indolizine derivatives as potent 5-HT4 partial agonists and their efficacy in animal models of cognition

246th National Meeting (2013)

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