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

Authors :: Nguyen, Diem N.
Paone, Daniel V.
Shaw, Anthony W.
Burgey, Christopher S.
Mosser, Scott D.
Johnston, Victor
Salvatore, Christopher A.
Leonard, Yvonne M.
Miller-Stein, Cynthia M.
Kane, Stefanie A.
Koblan, Kenneth S.
Vacca, Joseph P.
Graham, Samuel L.
Williams, Theresa M.
Source :: Bioorganic & Medicinal Chemistry Letters. Jan2008, Vol. 18 Issue 2, p755-758. 4p.
Publication Year :: 2008
Abstract: 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. [Copyright &y& Elsevier]

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