Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents.
Bioorg Med Chem Lett
; 26(15): 3453-6, 2016 08 01.
Article
em En
| MEDLINE
| ID: mdl-27372809
ABSTRACT
Novel 1,4-benzodiazepines, endowed with a Michael acceptor moiety, were designed taking advantage of a computational prediction of their pharmacokinetic parameters. Among all the synthesized derivatives, we identified a new lead compound (i.e., 4a), bearing a vinyl ketone warhead and endowed with a promising antitrypanosomal activity against Trypanosoma brucei brucei (IC50=5.29µM), coupled with a lack of cytotoxicity towards mammalian cells (TC50 >100µM).
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tripanossomicidas
/
Trypanosoma brucei brucei
/
Benzodiazepinas
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
Itália