Structure-based approach to falcipain-2 inhibitors: synthesis and biological evaluation of 1,6,7-trisubstituted dihydroisoquinolines and isoquinolines.
Bioorg Med Chem
; 11(10): 2293-9, 2003 May 15.
Article
em En
| MEDLINE
| ID: mdl-12713840
ABSTRACT
1,4,7-Trisubstituted isoquinolines were designed, synthesized and evaluated for their inhibition against Plasmodium falciparum cysteine protease falcipain-2. The 1-benzyloxyphenyl-dihydroisoquinoline and -isoquinoline derivatives were found to exhibit better activity against falcipain-2 than their corresponding 1-hydroxyphenyl or 1-methoxyphenyl analogues. The docking scores correlate with the IC(50) values of compounds and give a high coefficient correlation of 0.94.
Buscar no Google
Base de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
/
Inibidores de Cisteína Proteinase
/
Isoquinolinas
/
Antimaláricos
Idioma:
En
Ano de publicação:
2003
Tipo de documento:
Article