Calcitonin gene-related peptide (CGRP) receptor antagonists: novel aspartates and succinates.

Guanglin Luo, Ling Chen, Sokhom S Pin, Cen Xu, Charles M Conway, John E Macor, Gene M Dubowchik

Molecular Sciences and Candidate Optimization, Neuroscience Discovery Biology, Bristol-Myers Squibb Research & Development, Wallingford, CT 06492, USA. guanglin.luo@bms.com

Bioorganic & medicinal chemistry letters 2012 Apr 15

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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. Copyright © 2012 Elsevier Ltd. All rights reserved.

Citation

Guanglin Luo, Ling Chen, Sokhom S Pin, Cen Xu, Charles M Conway, John E Macor, Gene M Dubowchik. Calcitonin gene-related peptide (CGRP) receptor antagonists: novel aspartates and succinates. Bioorganic & medicinal chemistry letters. 2012 Apr 15;22(8):2912-6