Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 2 de 2
Filtrar
Añadir filtros








Intervalo de año
1.
Acta Pharmaceutica Sinica ; (12): 1054-1057, 2007.
Artículo en Chino | WPRIM | ID: wpr-268234

RESUMEN

Bicyclol is a new generation of anti-hepatitis drug with China's own intellectual property rights. The chemical structure of bicyclol is new and original. Pharmacological research showed that it has high clinical efficacy in treating chronic hepatitis (HBV) patients and lower side effects. Two metabolites of bicyclol have been isolated: M2 (4-hydroxy-4'-methoxy-5, 6, 5', 6'-bis (methylenedioxy)-2-hydroxylmethyl-2'-methoxycarbonyl biphenyl) and M3 (4'-hydroxy-4-methoxy-5, 6, 5', 6'-bis (methyl enedioxy)-2-hydroxylmethyl-2'-methoxycarbonyl biphenyl). To further study the mechanism, safety, and effectiveness of bicyclol, the M2 and M3 have been total synthesized. The synthesis route is as following: the carboxyl and phenolic hydroxyl group of the aromatic bromide had been separately protected by bromobenzyl, coupling through the intermolecular asymmetric Ullmann reaction and then catalyst hydrogenated, borane reducted, two metabolites of bicyclol M2 and M3 were obtained. The structures were determined by IR, 1H NMR, HRMS. Comparison of hepatoprotective activity of bicyclol and the two metabolites on experimental liver injury, the potency of the metabolites were lower than that of bicyclol.


Asunto(s)
Animales , Ratones , Alanina Transaminasa , Sangre , Benzodioxoles , Química , Farmacología , Compuestos de Bifenilo , Metabolismo , Intoxicación por Tetracloruro de Carbono , Enfermedad Hepática Inducida por Sustancias y Drogas , Sangre
2.
Acta Pharmaceutica Sinica ; (12): 221-224, 2006.
Artículo en Chino | WPRIM | ID: wpr-271472

RESUMEN

<p><b>AIM</b>To study the different biological activities of the enantiomers of the anti-hepatitis drug (+/-)-bicyclol, the (+/-)-bicyclol was resolved.</p><p><b>METHODS</b>By being treated with optically active alkaloid, the two diastereoisomers alkaloid salts of the compound could be obtained, separately. After decomposing and methylating, they were transformed separately into (-)-bicyclol and (+)-bicyclol.</p><p><b>RESULTS</b>The two enantiomers of bicyclol were determined by melting point, [alpha]D, 1H NMR, MS and chiral column HPLC.</p><p><b>CONCLUSION</b>Comparison of hepatoprotective action of racemic bicyclol and (-)-, (+)-bicyclol on experimental liver injury, the effect of (-)-bicyclol was two times more potent than that of racemic bicyclol and the potency of (+)-bicyclol was much less than that of the racemate.</p>


Asunto(s)
Animales , Ratones , Alanina Transaminasa , Sangre , Aspartato Aminotransferasas , Sangre , Compuestos de Bifenilo , Química , Farmacología , Intoxicación por Tetracloruro de Carbono , Enfermedad Hepática Inducida por Sustancias y Drogas , Sangre , Estructura Molecular , Rotación Óptica , Estereoisomerismo
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA