title: Evaluation of WO 2012/177618 A1 and US-2014/0179750 A1: novel small molecule antagonists of prostaglandin-E2 receptor EP2.
abstract: Recent studies underscore that prostaglandin-E2 exerts mostly proinflammatory effects in chronic CNS and peripheral disease models, mainly through a specific prostanoid receptor EP2. However, very few highly characterized EP2 receptor antagonists have been reported until recently, when Pfizer and Emory University published two distinct classes of EP2 antagonists with good potency, selectivity and pharmacokinetics. The purpose of this article is to evaluate recently published patents WO 2012/177618 A1 and US-2014/0179750 A1 from Emory, which describe a number of cinnamic amide- and amide-derivatives as a potent antagonists of EP2 receptor, and their neuroprotective effects in in vitro and in an in vivo model. A selected compound from this patent(s) also attenuates prostate cancer cell growth and invasion in vitro, suggesting these compounds should be developed for therapeutic use.
authors.affiliation: Emory University School of Medicine, Department of Pharmacology , 1510 Clifton Rd, Atlanta, GA 30322 , USA +1 404 727 7393 ; +1 404 727 0365 ; tganesh@emory.edu.
authors.forename: Thota
authors.initials: T
authors.lastname: Ganesh
mesh_terms: D000577:Amides / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D015232:Dinoprostone / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D008297:Male; D018696:Neuroprotective Agents / Q000494:pharmacology*; D010330:Patents as Topic; D011471:Prostatic Neoplasms / Q000188:drug therapy / Q000473:pathology; D058307:Receptors, Prostaglandin E, EP2 Subtype / Q000037:antagonists & inhibitors*
chemical_list: D000577:Amides; D018696:Neuroprotective Agents; D058307:Receptors, Prostaglandin E, EP2 Subtype; D015232:Dinoprostone
keywords: amides; anti-cancer; cinnamic amides; competitive antagonism; neuroinflammation; neuroprotection; status epilepticus