Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application.
Bioorg Med Chem Lett
; 20(7): 2270-4, 2010 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-20188549
ABSTRACT
PDE4 inhibitors are a validated approach as anti-inflammatory agents but are limited by systemic side effects including emesis. We report a soft-drug strategy incorporating a carboxylic ester group into boron-containing PDE4 inhibitors leading to the discovery of a series of benzoxaborole compounds with good potency (for example IC(50)=47 nM of compound 2) and low emetic activity. These compounds are intended for dermatological use further limiting possible systemic side effects.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Boro
/
Nucleotídeo Cíclico Fosfodiesterase do Tipo 4
/
Inibidores da Fosfodiesterase 4
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Anti-Inflamatórios
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article