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在药物分子设计中,等排置换是一种重要的局部结构改造策略。本文按改造对象的结构从简单到复杂的程度,将等排置换进行新的分类,主要包括原子或基团的等排置换、官能团的等排置换,以及环的等排置换。通过理论分析和代表性实例介绍,展示了等排置换的策略在提高化合物的活性和选择性、降低毒性和不良反应、改善药动学性质,以及增加化合物新颖性等方面的广泛应用。
In drug molecule design, isochronism is an important strategy of local structural transformation. In this paper, according to the structure of the object of transformation from simple to complex degree, the isochronism will be changed into new classification, including the replacement of isoms or groups, the replacement of functional groups, and the replacement of rings. Through theoretical analysis and representative examples, the strategy of isosorbide exchange is shown to be widely used in improving the activity and selectivity of compounds, reducing the toxicity and adverse reactions, improving the pharmacokinetic properties and increasing the novelty of compounds.