Your browser doesn't support javascript.
loading
Calcitonin gene-related peptide (CGRP) receptor antagonists: novel aspartates and succinates.
Luo, Guanglin; Chen, Ling; Pin, Sokhom S; Xu, Cen; Conway, Charles M; Macor, John E; Dubowchik, Gene M.
Affiliation
  • Luo G; Molecular Sciences and Candidate Optimization, Neuroscience Discovery Biology, Bristol-Myers Squibb Research & Development, Wallingford, CT 06492, USA. guanglin.luo@bms.com
Bioorg Med Chem Lett ; 22(8): 2912-6, 2012 Apr 15.
Article in En | MEDLINE | ID: mdl-22429471
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.
Subject(s)
Fulltext
Add to My VHL
Print
XML
PubMed Links
Search on Google

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Succinates / Aspartic Acid / Calcitonin Gene-Related Peptide Receptor Antagonists Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2012 Document type: Article Affiliation country: United States Country of publication: United kingdom
Fulltext
Add to My VHL
Print
XML
PubMed Links
Search on Google

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Succinates / Aspartic Acid / Calcitonin Gene-Related Peptide Receptor Antagonists Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2012 Document type: Article Affiliation country: United States Country of publication: United kingdom