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Lead compound optimization strategy (4)--improving blood-brain barrier permeability through structural modification / 药学学报
Acta Pharmaceutica Sinica ; (12): 789-799, 2014.
Artículo en Chino | WPRIM | ID: wpr-245013
ABSTRACT
Blood-brain barrier is a natural protection for human body. It protects central nervous system from the interruption and damage of xenobiotics. However, it prevents potential drugs aimed at central nervous system, thus becomes an obstruction for the development of central nervous system drugs. The recent development of blood-brain barrier permeability research and several lead optimization strategies to improve blood-brain barrier permeability are reviewed. These structure optimization methods include increasing lipophilicity, reducing hydrogen bond doners, simplifying molecule, increasing rigidity, lowering polar surface area, avoiding acid group, prodrug strategy, modifying into active transporter's substrates, as well as avoiding P-glycoprotein recognized structures.
Asunto(s)
Texto completo: Disponible Índice: WPRIM (Pacífico Occidental) Asunto principal: Permeabilidad / Transporte Biológico / Farmacocinética / Barrera Hematoencefálica / Diseño de Fármacos / Xenobióticos / Sistema Nervioso Central / Fármacos del Sistema Nervioso Central / Miembro 1 de la Subfamilia B de Casetes de Unión a ATP / Metabolismo Límite: Humanos Idioma: Chino Revista: Acta Pharmaceutica Sinica Año: 2014 Tipo del documento: Artículo

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Texto completo: Disponible Índice: WPRIM (Pacífico Occidental) Asunto principal: Permeabilidad / Transporte Biológico / Farmacocinética / Barrera Hematoencefálica / Diseño de Fármacos / Xenobióticos / Sistema Nervioso Central / Fármacos del Sistema Nervioso Central / Miembro 1 de la Subfamilia B de Casetes de Unión a ATP / Metabolismo Límite: Humanos Idioma: Chino Revista: Acta Pharmaceutica Sinica Año: 2014 Tipo del documento: Artículo