PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
Bioorg Med Chem Lett
; 17(3): 789-92, 2007 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-17107795
ABSTRACT
A method to access totally new analogues of tadalafil was explored. The Buchwald reaction was adapted and used to replace the methyl group of tadalafil by various aryl groups. Inhibition potencies on PDE5 of these analogues were determined and proved to be comparable to the one of tadalafil. Using the same route, compounds with the same level of activity but improved water solubility were produced by introducing a pyridine or a pyrimidine ring. This original route also opens access to new unpatented compounds.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Carbolinas
/
3',5'-GMP Cíclico Fosfodiesterases
/
Inibidores Enzimáticos
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2007
Tipo de documento:
Article
País de afiliação:
França