Preparation, crystal structure and prodrug studies of genistein benzensulfonate
4'-ethyl-7-phenylsulfonylgenistein (EPG, 3), a potential prodrug for genistein (1), was synthesized in high yield and its crystal structure was reported firstly. It possesses better physical and chemical properties such as solubility, lipid/water partition coefficient, LogP, and hydrolysis kine...
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| Autores principales: | , , |
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| Formato: | Articulo Comunicacion |
| Lenguaje: | Inglés |
| Publicado: |
2011
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| Materias: | |
| Acceso en línea: | http://sedici.unlp.edu.ar/handle/10915/8322 http://www.latamjpharm.org/resumenes/30/7/LAJOP_30_7_2_7.pdf |
| Aporte de: |
| Sumario: | 4'-ethyl-7-phenylsulfonylgenistein (EPG, 3), a potential prodrug for genistein (1), was synthesized in high yield and its crystal structure was reported firstly. It possesses better physical and chemical properties such as solubility, lipid/water partition coefficient, LogP, and hydrolysis kinetics than its original form. The LogP value (2.07) and the half-life of the hydrolysis value (13.4 h) show that its oral bioavailability is possibly improved evidently compared with that of genistein. These results indicate that EPG can be considered a potential prodrug for genistein. |
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