期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 22, 页码 6827-6830出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.08.105
关键词
CGRP; Calcitonin gene-related peptide; Antagonist
A previously utilized quinoline-for-N-phenylamide replacement strategy was employed against a central amide in a novel class of CGRP receptor antagonists. A unique and unexpected substitution pattern was ultimately required to maintain reasonable affinity for the CGRP receptor, while at the same time predicting acceptable heterocycle positioning for related analogs. Subsequently, specific quinoline and naphthyridine compounds were prepared which supported these structural predictions by displaying CGRP binding affinities in the 0.037-0.15 nM range. (C) 2010 Elsevier Ltd. All rights reserved.
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