| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369324 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
An oxidation product (5) formed during the synthesis of BIBN-4096BS (1) was found to be a potent CGRP antagonist (IC50 = 0.11 nM). While 5 was found to be ten-fold less potent than 1, another analog 8 with lower molecular weight containing the oxidized fragment demonstrated twenty-fold higher activity than its parent 7. Alternative conditions which preclude the formation of the oxidation product are described. The activities of 1, 5, 7 and 8 in functional cAMP assay are also discussed.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Bireshwar Dasgupta, Edward Kozlowski, Daniel R. Schroeder, John R. Torrente, Cen Xu, Sokhom Pin, Charlie M. Conway, Gene M. Dubowchik, John E. Macor, Vivekananda M. Vrudhula,