| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369517 | Bioorganic & Medicinal Chemistry Letters | 2016 | 4 Pages |
Abstract
Calcitonin gene-related peptide (CGRP) is a potent neuropeptide implicated in the pathophysiology of migraine. In the course of seeking CGRP antagonists with improved oral bioavailability, metabolic stability, and pharmacokinetic properties, lower molecular weight, structurally simpler piperidine and piperazine analogs of BMS-694153 were prepared. Several were found to have nM binding affinity in vitro. The synthesis and SAR of these substituted piperidine and piperazine CGRP antagonists are discussed.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Rita L. Civiello, Xiaojun Han, Brett R. Beno, Prasad V. Chaturvedula, John J. Herbst, Cen Xu, Charles M. Conway, John E. Macor, Gene M. Dubowchik,