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

…, C Xu, CM Conway, JE Macor, GM Dubowchik

Index: Luo, Guanglin; Chen, Ling; Pin, Sokhom S.; Xu, Cen; Conway, Charles M.; MacOr, John E.; Dubowchik, Gene M. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 8 p. 2912 - 2916

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Citation Number: 2

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.