Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: part 3.
Bioorg Med Chem Lett
; 23(13): 3798-801, 2013 Jul 01.
Article
em En
| MEDLINE
| ID: mdl-23711919
ABSTRACT
In an effort to develop potent and selective inhibitors toward ACAT2, structure-activity relationship studies were carried out using derivatives based on pyripyropene A (PPPA, 1). In particular, we investigated the possibility of introducing appropriate 1,11-O-benzylidene and 7-O-substituted benzoyl moieties into PPPA (1). The new o-substituted benzylidene derivatives showed higher selectivity for ACAT2 than PPPA (1). Among them, 1,11-O-o-methylbenzylidene-7-O-p-cyanobenzoyl PPPA derivative 7q and 1,11-O-o,o-dimethylbenzylidene-7-O-p-cyanobenzoyl PPPA derivative 7z proved to be potent ACAT2 inhibitors with unprecedented high isozyme selectivity.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Sesquiterpenos
/
Esterol O-Aciltransferase
/
Inibidores Enzimáticos
Limite:
Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article