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2014
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Jiang, Jianxiong
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Article
Lead Optimization Studies of Cinnamic Amide EP2 Antagonists
by
Thota Ganesh
;
Jianxiong Jiang
;
Myung-Soon Yang
;
Raymond Dingledine
2014
Subjects
Health Sciences, Pharmacology
Health Sciences, Pharmacy
Health Sciences, General
File Download
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Abstract:
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Prostanoid receptor EP2 can play a proinflammatory role, exacerbating disease pathology in a variety of central nervous system and peripheral diseases. A highly selective EP2 antagonist could be useful as a drug to mitigate the inflammatory consequences of EP2 activation. We recently identified a cinnamic amide class of EP2 antagonists. The lead compound in this class (5d) displays anti-inflammatory and neuroprotective actions. However, this compound exhibited moderate selectivity to EP2 over the DP1 prostanoid receptor (∼10-fold) and low aqueous solubility. We now report compounds that display up to 180-fold selectivity against DP1 and up to 9-fold higher aqueous solubility than our previous lead. The newly developed compounds also display higher selectivity against EP4 and IP receptors and a comparable plasma pharmacokinetics. Thus, these compounds are useful for proof of concept studies in a variety of models where EP2 activation is playing a deleterious role. © 2014 American Chemical Society.