Application of carbamyl in structural optimization
Application of carbamyl in structural optimization
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氨甲酰在结构优化中的应用
DOI：
10.1016/j.bioorg.2020.103757
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发表时间：
2020
影响因子：
5.1
通讯作者：
Yongshou Tian
中科院分区：
文献类型：
--
作者：
Kuanglei Wang;Hongxi Zhu;Hongqian Zhao;Kun Zhang;Yongshou Tian
氨甲酰基被认为是药物化学中的特权结构。它具有抗菌、抗癌、抗癫痫等广泛的生物活性，最好的证据是一些已上市的含氨甲酰的药物。氨甲酰基由伯胺和羰基组成，分别作为氢键供体和氢受体与靶位残基结合，有利于提高药理活性。在其他情况下，引入的氨基甲酰基改善了药物样性质，包括口服生物利用度。本文综述了含氨甲酰的药物及其在结构优化中的应用，以提高药物的活性或/和类药物性质。
Carbamyl is considered a privileged structure in medicinal chemistry. It has a wide range of biological activities such as antimicrobial, anticancer, anti-epilepsy, for which the best evidence is a number of marketed carbamyl-containing drugs. Carbamyl is formed of primary amine and carbonyl moieties that act as hydrogen bond donors and hydrogen acceptors with residues of targets respectively, which are benefit for improving pharmacological activities. In other cases, the introduced carbamyl improves drug-like properties including oral bioavailability. In this review, we introduce the carbamyl-containing drugs and the application of carbamyl in structural optimization as a result of enhancing activities or/and drug-like properties.