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OALib Journal期刊
ISSN: 2333-9721
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基于骨架跃迁和药物拼接所确立的新型二肽基肽酶iv抑制剂
, PP. 61-67
Keywords: 2型糖尿病,dpp-iv抑制剂,骨架跃迁,药物拼接
Abstract:
截至目前，已有7个二肽基肽酶iv（dpp-iv）抑制剂成为抗糖尿病新药，它们的结构差异和内在关联性为进一步的结构修饰提供了新的思路。本研究针对阿格列汀和利那列汀的结构特征，采用骨架跃迁及药物拼接的原理，快速得到了新型的dpp-iv抑制剂8g（ic50=4.9nmol·l-1），其活性和选择性均接近于上市新药。因此，运用经典的药物化学策略，对基于同一靶标的上市药物实施分子操作，可以有效地产生新型的活性分子。
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