Flavones. 3. Synthesis, biological activities, and conformational analysis of isoflavone derivatives and related compounds.
J Med Chem
; 35(19): 3519-25, 1992 Sep 18.
Article
en En
| MEDLINE
| ID: mdl-1404232
A series of 2-alkylisoflavone derivatives 1 was prepared with the intent to study the importance of the phenyl group (at the 3-position) of the isoflavone in imparting antihypertensive activity and the substitution effects at the 2-position of isoflavone. With the exception of the 2-isopropyl analog, the antihypertensive activity of these compounds appears to have a slow onset and long duration. None of the analogs appears better than the corresponding flavone (3) and 3-phenylflavone (2) analogs. An unsuccessful attempt to correlate the relationship between antihypertensive activity and the calculated torsional angle of C2-C3-C1'-C2' is discussed. Antiinflammatory activities of these compounds along with 7-(oxypropylamine)flavones were also evaluated and found to be not very potent. The antiinflammatory activity appears to be sensitive to steric effects of the alkyl group on the nitrogen and of substituents at the 2-position of the isoflavones, while the hydroxyl group of the propanolamine side chain is not essential.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Flavonoides
/
Antihipertensivos
Límite:
Animals
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
1992
Tipo del documento:
Article
Pais de publicación:
Estados Unidos