Author/Authors :
Diem N. Nguyen، نويسنده , , Daniel V. Paone، نويسنده , , Anthony W. Shaw، نويسنده , , Christopher S. Burgey، نويسنده , , Scott D. Mosser، نويسنده , , Victor Johnston، نويسنده , , Christopher A. Salvatore، نويسنده , , Yvonne M. Leonard، نويسنده , , Cynthia M. Miller-Stein، نويسنده , , Stefanie A. Kane، نويسنده , , Kenneth S. Koblan، نويسنده , , Joseph P. Vacca، نويسنده , , Samuel L. Graham، نويسنده , , Theresa M. Williams، نويسنده ,
Abstract :
In our effort to find potent, orally bioavailable CGRP receptor antagonists for the treatment of migraine, a novel series based on a pyridinone template was investigated. After optimizing the privileged structure and the placement of the attached phenyl ring, systematic SAR was carried out on both the N-alkyl and C-5 aryl substituents. Several analogs with good potency and pharmacokinetic profiles were identified.
