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中文摘要：
含氟药物在临床治疗药物中占有相当比重.将氟原子或含氟基团引入到小分子药物中,是药物化学结构改造的重要研究策略之一.综述了氟原子在药物分子设计中的应用,氟原子或含氟基团的引入可以调节药物小分子的物理化学特性,改变小分子的药代动力学性质,提高药物的生物利用度;通过影响化合物的构象,增强配体与靶标蛋白的相互结合能力以及对其它靶标蛋白的选择性;通过阻断易代谢位点进而提高药物代谢稳定性等.
英文摘要：
Fluorinated compounds comprise a substantial proportion in the therapeutic drugs.It is an important strategy to introduce fluorine and fluorinated substitutes in the small molecule for structure-based medicinal chemistry.They can modulate the physicochemical and pharmacokinetic properties to improve bioavailability,alter the conformation of a molecule to enhance the selectivities and binding affinity to target proteins,and block metabolically labile sites to increase the metabolic stability of drugs.
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