Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1361301 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
Novel aspartate and succinate CGRP full antagonists were identified through core modification of a potent lead CGRP antagonist, BMS-694153. While aspartates were much less active and had a flat SAR, some of the succinates were very potent CGRP full antagonists and matched the potency of BMS-694153. The most potency resides in the S enantiomer as demonstrated through an asymmetric synthesis.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Guanglin Luo, Ling Chen, Sokhom S. Pin, Cen Xu, Charles M. Conway, John E. Macor, Gene M. Dubowchik,