Discovery of a subnanomolar and selective spirocyclic agonist of the glucocorticoid receptor.
Eur J Med Chem
; 161: 354-363, 2019 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-30384041
ABSTRACT
Pure diastereomeric spirocyclic analogs of fluorocortivazol were conveniently prepared by a short and efficient synthetic sequence recently developed in our laboratory. The structures and conformations of several key products were confirmed by single crystal X-ray diffraction analysis. Conformational assignments were also supported by DFT calculations. Biological evaluation led to the identification of a highly potent hGR agonist with excellent anti-inflammatory effects in the subnanomolar range. All tested compounds from this series were also selective versus the progesterone receptor.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos de Espiro
/
Receptores de Glucocorticoides
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Anti-Inflamatórios não Esteroides
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Descoberta de Drogas
Limite:
Humans
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article