Lead optimization of a sulfonylurea-based piperazine pyridazinone series of glucan synthase inhibitors.
Bioorg Med Chem Lett
; 22(14): 4896-9, 2012 Jul 15.
Article
em En
| MEDLINE
| ID: mdl-22687744
ABSTRACT
The structure-activity relationship studies of a novel sulfonylurea series of piperazine pyridazine-based small molecule glucan synthase inhibitors is described. The optimization of PK profiles within the series led to the discovery of several compounds with improved pharmacokinetic profiles which demonstrated in vitro potency against clinically relevant strains. However, the advancement of compounds from this series into a non-lethal systemic fungal infection model failed to show in vivo efficacy.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Piridazinas
/
Compostos de Sulfonilureia
/
Inibidores Enzimáticos
/
Glucosiltransferases
/
Chumbo
/
Antifúngicos
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article