Q4 · MEDICINE
Article
Author: Salvi, Matteo ; Shirsath, Vikas ; Piepoli, Tiziana ; Bhimani, Kanji ; Pucci, Sabrina ; Canciani, Luca ; Mennuni, Laura ; Zerbi, Silvia ; Stasi, Luigi Piero ; Ferioli, Cristian ; Kaswala, Mehul ; Caselli, Gianfranco ; Colace, Fabrizio ; Borriello, Manuela ; Zanelli, Tiziano
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.