2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2011 Nov 1;21(21):6336-40. doi: 10.1016/j.bmcl.2011.08.102.
Luigi Piero Stasi 1,  Kanji Bhimani,  Manuela Borriello,  Luca Canciani,  Gianfranco Caselli,  Fabrizio Colace,  Cristian Ferioli,  Mehul Kaswala,  Laura Mennuni,  Tiziana Piepoli,  Sabrina Pucci,  Matteo Salvi,  Vikas Shirsath,  Tiziano Zanelli,  Silvia Zerbi
Affiliations

Affiliation

  • 1 Rottapharm Madaus, Medicinal Chemistry Department, via Valosa di Sopra 9, Monza 20900, Italy. luigi.stasi@rottapharm.com
PMID: 21930381 DOI: 10.1016/j.bmcl.2011.08.102
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.

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