Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371896 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
A novel class of CGRP receptor antagonists was rationally designed by modifying a highly potent, but structurally complex, CGRP receptor antagonist. Initial modifications focused on simplified structures, with increased flexibility. Subsequent to the preparation of a less-potent but more flexible lead, classic medicinal chemistry methods were applied to restore high affinity (compound 22, CGRP Ki = 0.035 nM) while maintaining structural diversity relative to the lead. Good selectivity against the closely related adrenomedullin-2 receptor was also achieved.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Michael R. Wood, Kathy M. Schirripa, June J. Kim, Amy G. Quigley, Craig A. Stump, Ian M. Bell, Rodney A. Bednar, John F. Fay, Joseph G. Bruno, Eric L. Moore, Scott D. Mosser, Shane Roller, Christopher A. Salvatore, Stefanie A. Kane, Joseph P. Vacca,