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Bioorg Med Chem Lett. 2010 Nov 15;20(22):6827-30. doi: 10.1016/j.bmcl.2010.08.105. Epub 2010 Aug 26.

Novel CGRP receptor antagonists from central amide replacements causing a reversal of preferred chirality.

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Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 4, 770 Sumneytown Pike, West Point, PA 19486, United States.


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.

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