Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate.
Bioorg Med Chem Lett
; 21(4): 1141-5, 2011 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-21256008
ABSTRACT
Following the discovery that hydroxylated derivative 3 (Fig. 1) was one of the oxidative metabolites of the original lead 1, it was found that hydroxylated compound 4 possesses higher in vitro anti-HIV potency than the corresponding non-hydroxylated compound 2. Structural hybridation of 4 with the orally available analog 5 resulted in another orally-available spirodiketopiperazine CCR5 antagonist 6a that possesses more favorable pharmaceutical profile for use as a drug candidate.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos de Espiro
/
Fármacos Anti-HIV
/
Dicetopiperazinas
/
Antagonistas dos Receptores CCR5
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article