Structure-Activity Relationship Studies of EP2 Antagonists for Aqueous Solubility Enhancement Restricted; Files Only
Matthews, Sigrid (Spring 2024)
Abstract
Over the past decade, EP2 antagonism has emerged as a promising treatment for neuroinflammation and neurodegenerative diseases including Alzheimer’s, Parkinson’s, epilepsy, and traumatic brain injury. Following the discovery of selective antagonists, proof of concept in animals supports the continued pursuit of a clinical candidate with improved solubility, brain permeability, and half-life. Following structure-activity relations of previous successful compounds, derivatives were developed with varying middle and final rings in an attempt to optimize the candidates. Two scaffolds were followed resulting in the synthesis of two novel antagonists and partial synthesis of multiple others. Of these compounds, one had moderate potency and low solubility, while the other had improved potency and selectivity against the DP1 receptor.
Table of Contents
Abstract 1
Introduction 2
Goals 8
Results 9
Discussion 14
Experimental Methods 19
Characterization 23
References 33
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