Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole.
Bioorg Med Chem Lett
; 18(3): 963-8, 2008 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-18207393
ABSTRACT
Design, synthesis and conformational analysis of few imidazole and oxazole as bioisosters of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) 2 is reported. Computer assisted conformational analysis gave a direct clue for the loss of CB1 antagonistic activity of the ligands without a fine docking simulation for the homology model.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Oxazóis
/
Pirazóis
/
Sulfonamidas
/
Modelos Moleculares
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Receptor CB1 de Canabinoide
/
Imidazóis
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article