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. 2012 Apr 15;22(8):2912-6.
doi: 10.1016/j.bmcl.2012.02.066. Epub 2012 Mar 3.

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

Guanglin Luo  1 , Ling Chen, Sokhom S Pin, Cen Xu, Charles M Conway, John E Macor, Gene M Dubowchik
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Calcitonin gene-related peptide (CGRP) receptor antagonists: novel aspartates and succinates

Guanglin Luo et al. Bioorg Med Chem Lett. .

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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