| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1361302 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
In our continuing efforts to identify CGRP receptor antagonists that can be dosed orally for the treatment of migraine headache, we have investigated a pyridine bioisosteric replacement of a polar amide portion of a previous lead compound, BMS-694153. Pyridine derivatives were discovered and their SAR was studied. Some of them showed excellent binding potency. However, oral bioavailability was low, even for compounds with good Caco-2 cell permeability.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Guanglin Luo, Ling Chen, Rita Civiello, Sokhom S. Pin, Cen Xu, Walter Kostich, Michelle Kelley, Charles M. Conway, John E. Macor, Gene M. Dubowchik,