Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template.

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.