Structure-activity relationships in platelet-activating factor (PAF antagonists). 6. Synthesis and in vitro antagonistic activities of 2-substituted 5-oxotetrahydrofurans.
J Lipid Mediat
; 5(1): 23-40, 1992 Feb.
Article
en En
| MEDLINE
| ID: mdl-1449553
ABSTRACT
The synthesis of 2,5-disubstituted tetrahedrofuran compounds as potential in vitro PAF antagonists is described. Results demonstrate that the structural requirements for potent PAF antagonist activity are a moderate lipophilic group or a trimethoxyphenyl group in position-5, and a long aliphatic chain terminated by a cationic polar head in position-2. The cis-trans configuration does not induce any difference in biological activity. Some conformational features of the putative PAF receptor are proposed in light of the present findings.
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Base de datos:
MEDLINE
Asunto principal:
Inhibidores de Agregación Plaquetaria
/
Factor de Activación Plaquetaria
/
Furanos
Límite:
Animals
Idioma:
En
Revista:
J Lipid Mediat
Asunto de la revista:
BIOQUIMICA
Año:
1992
Tipo del documento:
Article
País de afiliación:
Francia