Synthesis and SAR studies on azetidine-containing dipeptides as HCMV inhibitors.
Bioorg Med Chem
; 19(3): 1155-61, 2011 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-21256035
SAR studies on an azetidine-containing dipeptide prototype inhibitor of HCMV are described. Three series of structurally modified analogues, involving substitutions at the N- and C-terminus, and at the C-terminal side-chain were synthesized and evaluated for antiviral activity. Aliphatic or no substituents at the C-carboxamide group, an aliphatic C-terminal side-chain, as well as a benzyloxycarbonyl moiety at the N-terminus were absolute requirements for anti-HCMV activity. The conformational restriction induced by the 2-azetidine residue into the dipeptide derivatives, identified by (1)H NMR as a γ-type reverse turn, seems to have influence on the activity of these molecules.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Azetidinas
/
Infecções por Citomegalovirus
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Citomegalovirus
/
Dipeptídeos
Limite:
Humans
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article