title: Synthesis, pharmacophore modeling and in vitro activity of 10,11-dihydrodibenzo[b,f]oxepine-4-carboxamide derivatives as novel and potent antagonists of the prostaglandin EP4 receptor.
abstract: The construction of a EP(4) antagonists pharmacophore model and the discovery of a highly potent oxepinic series of EP(4) antagonists is discussed. Compound 1a exhibits an excellent selectivity profile toward EP(2) receptor subtype and low cytochrome P450 inhibition potential.
authors.affiliation: Rottapharm Madaus, Medicinal Chemistry Department, via Valosa di Sopra 9, Monza 20900, Italy. luigi.stasi@rottapharm.com
authors.forename: Luigi Piero
authors.initials: LP
authors.lastname: Stasi
authors.forename: Kanji
authors.initials: K
authors.lastname: Bhimani
authors.forename: Manuela
authors.initials: M
authors.lastname: Borriello
authors.forename: Luca
authors.initials: L
authors.lastname: Canciani
authors.forename: Gianfranco
authors.initials: G
authors.lastname: Caselli
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Colace
authors.forename: Cristian
authors.initials: C
authors.lastname: Ferioli
authors.forename: Mehul
authors.initials: M
authors.lastname: Kaswala
authors.forename: Laura
authors.initials: L
authors.lastname: Mennuni
authors.forename: Tiziana
authors.initials: T
authors.lastname: Piepoli
authors.forename: Sabrina
authors.initials: S
authors.lastname: Pucci
authors.forename: Matteo
authors.initials: M
authors.lastname: Salvi
authors.forename: Vikas
authors.initials: V
authors.lastname: Shirsath
authors.forename: Tiziano
authors.initials: T
authors.lastname: Zanelli
authors.forename: Silvia
authors.initials: S
authors.lastname: Zerbi
mesh_terms: D001584:Benzoxepins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D006801:Humans; D066298:In Vitro Techniques; D008958:Models, Molecular; D058309:Receptors, Prostaglandin E, EP4 Subtype / Q000037:antagonists & inhibitors*
chemical_list: C569520:10,11-dihydrodibenzo(b,f)oxepine-4-carboxamide; D001584:Benzoxepins; D058309:Receptors, Prostaglandin E, EP4 Subtype