title: Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.
abstract: Replacement of the hydroxy cyclopentanone ring in PGE(2) with chemically more stable heterocyclic rings and substitution of the unsaturated alpha-alkenyl chain with a metabolically more stable phenethyl chain led to the development of potent and selective analogs of PGE(2). Compound 10f showed the highest potency and selectivity for EP(4) the receptor.
authors.affiliation: Department of Medicinal Chemistry, EMD-Serono Research Institute, Inc., Rockland, MA 02370, USA. zhong.zhao@genzyme.com
authors.forename: Zhong
authors.initials: Z
authors.lastname: Zhao
authors.forename: Gian Luca
authors.initials: GL
authors.lastname: Araldi
authors.forename: Yufang
authors.initials: Y
authors.lastname: Xiao
authors.forename: Adulla P
authors.initials: AP
authors.lastname: Reddy
authors.forename: Yihua
authors.initials: Y
authors.lastname: Liao
authors.forename: Srinivasa
authors.initials: S
authors.lastname: Karra
authors.forename: Nadia
authors.initials: N
authors.lastname: Brugger
authors.forename: David
authors.initials: D
authors.lastname: Fischer
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Palmer
mesh_terms: D000818:Animals; D015232:Dinoprostone / Q000138:chemical synthesis* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D005260:Female; D006801:Humans; D051379:Mice; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D018078:Receptors, Prostaglandin E / Q000819:agonists* / Q000502:physiology; D058307:Receptors, Prostaglandin E, EP2 Subtype; D058309:Receptors, Prostaglandin E, EP4 Subtype
chemical_list: C545644:PTGER2 protein, human; C545650:PTGER4 protein, human; C545645:Ptger2 protein, mouse; C545651:Ptger4 protein, mouse; D011720:Pyrazoles; D018078:Receptors, Prostaglandin E; D058307:Receptors, Prostaglandin E, EP2 Subtype; D058309:Receptors, Prostaglandin E, EP4 Subtype; D015232:Dinoprostone