化学
氘
分子
氢-氘交换
药品
机制(生物学)
化学结构
小分子
组合化学
计算化学
药理学
有机化学
生物化学
氢
医学
哲学
物理
认识论
量子力学
作者
H.M. Chandra Mouli,Adithya Vinod,Shikha Kumari,Amit K. Tiwari,M.K. Kathiravan,V. Ravichandiran,Ramalingam Peraman
标识
DOI:10.1016/j.bioorg.2023.106490
摘要
In organic chemistry, the use of deuterium exchange as a tool to study the mechanism of chemical reaction has been well explored. Since two decades, the research focus on deuterated bioactive molecules has been gaining attention for investigating the therapeutic potential of deuterium replacement in a chemical structure. Recently, Food Drug Administration (FDA) approved the first deuterium-labeled drug "deutetrabenazine", and notified the deuterated drugs as new chemical entities (NCEs). Henceforth, the deuterium substitution driven structure activity relationship, preclinical pharmacokinetics, and toxicity studies were much initiated. Deuteration of a bioactive molecule often results in improved therapeutic efficacy due to the altered pharmacokinetic profile. This review provides a conceptual framework on the importance of deuterium atom in chemical structure of a drug, and its biological value in improved physiochemical properties, pharmacokinetics, biological target interaction, diagnosis, and toxicity. In addition, this review concisely updated the recent deuteration methods, chemical stability, challenges in drug development, deuterium-based imaging in diagnosis, and selected synthetic scheme of deuterated molecules.
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