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ID: ALA3286324
Journal: Bioorg Med Chem Lett
Title: Serendipitous oxidation product of BIBN4096BS: a potent CGRP receptor antagonist.
Authors: Dasgupta B, Kozlowski E, Schroeder DR, Torrente JR, Xu C, Pin S, Conway CM, Dubowchik GM, Macor JE, Vrudhula VM.
Abstract: An oxidation product (5) formed during the synthesis of BIBN-4096BS (1) was found to be a potent CGRP antagonist (IC50=0.11nM). 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.
CiteXplore: 24794104