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

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• 作者：Guanglin Luo ; ^{guanglin.luo@bms.com} ; Ling Chen ; Sokhom S. Pin ; Cen Xu ; Charles M. Conway ; John E. Macor ; Gene M. Dubowchik
• 关键词：CGRP antagonist ; Migraine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：15 April, 2012
• 年：2012
• 卷：22
• 期：8
• 页码：2912-2916
• 全文大小：3915 K

文摘

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.