Serendipitous oxidation product of BIBN4096BS: a potent CGRP receptor antagonist.
Bioorg Med Chem Lett
; 24(12): 2744-8, 2014 Jun 15.
Article
em En
| MEDLINE
| ID: mdl-24794104
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.
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Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Quinazolinas
/
Antagonistas do Receptor do Peptídeo Relacionado ao Gene de Calcitonina
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article