Synthesis and bioactivity of substituted alpha-aminobenzylphosphonate / 药学学报
Acta Pharmaceutica Sinica
; (12): 342-345, 2006.
Article
en Zh
| WPRIM
| ID: wpr-271430
Biblioteca responsable:
WPRO
ABSTRACT
<p><b>AIM</b>To search for some substituted alpha-amino phosphonates as leading compounds with the vasodilator effects.</p><p><b>METHODS</b>Target compounds were prepared from benzyl aldehyde, piperazine and diethyl phosphite using alcohol as solvent via Mannich-type reaction. In isolated rat aorta and in isolated guinea pig ileum, the vasodilator effects of compounds were investigated and evaluated whether they activated muscarine receptor.</p><p><b>RESULTS</b>Seven compounds of substituted alpha-amino phosphonates have been synthesized and identified by IR, 1H NMR and elemental analysis. Three of them, compound 2a, 2b and 2c have vasodilator activity and do not activate M receptor.</p><p><b>CONCLUSION</b>Two (2b and 2c) of them were found to have the notable vasodilator effect, and the rates of relaxing are (67 +/- 21) % and (82 +/- 18)%, separately. But they did not activate M receptors on ileum.</p>
Texto completo:
1
Base de datos:
WPRIM
Asunto principal:
Aorta
/
Farmacología
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Vasodilatación
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Vasodilatadores
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Bencilaminas
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Estructura Molecular
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Química
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Organofosfonatos
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Cobayas
/
Íleon
Límite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2006
Tipo del documento:
Article