| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375130 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
A novel series of potent CGRP receptor antagonists containing a central quinoline ring constraint was identified. The combination of the quinoline constraint with a tricyclic benzimidazolinone left hand fragment produced an analog with picomolar potency (14, CGRP Ki = 23 pM). Further optimization of the tricycle produced a CGRP receptor antagonist that exhibited subnanomolar potency (19, CGRP Ki = 0.52 nM) and displayed a good pharmacokinetic profile in three preclinical species.
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Related Topics
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Authors
Craig A. Stump, Ian M. Bell, Rodney A. Bednar, John F. Fay, Steven N. Gallicchio, James C. Hershey, Richard Jelley, Constantine Kreatsoulas, Eric L. Moore, Scott D. Mosser, Amy G. Quigley, Shane A. Roller, Christopher A. Salvatore, Steven S. Sharik,