Heterocyclic N-Oxides - An Emerging Class of Therapeutic Agents.
Heterocyclic N-Oxides - An Emerging Class of Therapeutic Agents.
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DOI：
10.2174/0929867322666150619104007
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发表时间：
2015
影响因子：
4.1
通讯作者：
Larionov OV
中科院分区：
文献类型：
--
作者：
Mfuh AM;Larionov OV
杂环N-氧化物已成为具有抗癌、抗菌、抗高血压、抗寄生虫、抗HIV、抗炎、除草、神经保护和促认知活性的有效化合物。N-氧化物基序已成功地应用于一些最近的药物开发项目。本文综述了这种支架在主流药物化学中的出现，重点介绍了杂环N-氧化物药物的发现，N-氧化物特异性作用机制，药物-受体相互作用以及这些化合物的合成途径。作为第一个审查，这一主题，涵盖了自20世纪50年代至今的发展，预计它将激发更广泛的实施，杂环N-氧化物基序的合理设计新的药物。
Heterocyclic N-oxides have emerged as potent compounds with anticancer, antibacterial, antihypertensive, antiparasitic, anti-HIV, anti-inflammatory, herbicidal, neuroprotective, and procognitive activities. The N-oxide motif has been successfully employed in a number of recent drug development projects. This review surveys the emergence of this scaffold in the mainstream medicinal chemistry with a focus on the discovery of the heterocyclic N-oxide drugs, N-oxide-specific mechanisms of action, drug-receptor interactions and synthetic avenues to these compounds. As the first review on this subject that covers the developments since 1950s to date, it is expected that it will inspire wider implementation of the heterocyclic N-oxide motif in the rational design of new medicinal agents.