| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375952 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
Rational modification of a previously identified spirohydantoin lead structure has identified a series of potent spiroazaoxindole CGRP receptor antagonists. The azaoxindole was found to be a general replacement for the hydantoin that consistently improved in vitro potency. The combination of the indanylspiroazaoxindole and optimized benzimidazolinones led to highly potent antagonists (e.g., 25, CGRP Ki = 40 pM). The closely related compound 27 demonstrated good oral bioavailability in dog and rhesus.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Craig A. Stump, Ian M. Bell, Rodney A. Bednar, Joseph G. Bruno, John F. Fay, Steven N. Gallicchio, Victor K. Johnston, Eric L. Moore, Scott D. Mosser, Amy G. Quigley, Christopher A. Salvatore, Cory R. Theberge, C. Blair Zartman, Xu-Fang Zhang,