Synthesis of an active hydroxylated glutethimide metabolite and some related analogs with sedative-hypnotic and anticonvulsant properties.
J Med Chem
; 18(7): 736-41, 1975 Jul.
Article
en En
| MEDLINE
| ID: mdl-1151995
ABSTRACT
Two synthetic pathways are described for the preparation of 4-hydroxy-2-ethyl-2-phenylglutarimide (2), an active hydroxylated metabolite of glutethimide (1). Fourteen other glutethimide analogs were also synthesized and tested for biological activity. Most of the analogs exhibited sedative-hypnotic properties and compound 2 possessed the greatest activity compared to the parent drug. 4-Amino-2-ethyl-2-phenylglutarimide and 4-hydroxy-2-ethyl-2-phenylglutaconimide (13) exhibited the greatest potential as anticonvulsant agents. The structure-activity relationships of the series are discussed.
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Banco de datos:
MEDLINE
Asunto principal:
Glutetimida
/
Hipnóticos y Sedantes
/
Anticonvulsivantes
Límite:
Animals
Idioma:
En
Año:
1975
Tipo del documento:
Article