Identification of 2,3-disubstituted pyridines as potent, orally active PDE4 inhibitors.
Bioorg Med Chem
; 21(18): 5851-4, 2013 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-23910988
ABSTRACT
A series of 2,3-disubstituted pyridines were synthesized and evaluated for their PDE4 inhibitory activity. We successfully modified undesirable cyano group of initial lead compound 2 to 4-pyridyl group with improvement of in vitro efficacy and optimized the position of nitrogen atoms in pyridine moiety and alkylene linker. The most potent compound showed significant efficacy in animal models of asthma and inflammation.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Piridinas
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Nucleotídeo Cíclico Fosfodiesterase do Tipo 4
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Inibidores da Fosfodiesterase 4
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Anti-Inflamatórios
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article