摘要
杂环氮氧化物已经成为一类具有抗肿瘤、抗菌、降血压、抗寄生虫、抗HIV、抗炎、除草、神经保护、强化认知等活性的化合物。最近,以氮氧为母核的化合物已被成功地应用在一些药物研发项目中。本文以主流药物化学为支点,主要综述了杂环氮氧化物类药物的发现,氮氧特别的作用机制,药物与受体的相互作用以及这些化合物的合成路径。这是关于该主题的第一篇综述,涵盖了自上世纪50年代以来的相关研究成果,预计将会激发更广泛的以杂环氮氧为母核新兴药的合理设计。
关键词: 杂环氮氧化物,一氧化氮模拟物,生物电子等排体,低氧血症,Xa因子抑制剂,凝血-级联型直接凝血酶抑制剂,抗南美洲锥虫病药,抗疟药
Current Medicinal Chemistry
Title:Heterocyclic N-Oxides - An Emerging Class of Therapeutic Agents
Volume: 22 Issue: 24
Author(s): A.M. Mfuh and O.V. Larionov
Affiliation:
关键词: 杂环氮氧化物,一氧化氮模拟物,生物电子等排体,低氧血症,Xa因子抑制剂,凝血-级联型直接凝血酶抑制剂,抗南美洲锥虫病药,抗疟药
摘要: 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.
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Cite this article as:
A.M. Mfuh and O.V. Larionov , Heterocyclic N-Oxides - An Emerging Class of Therapeutic Agents, Current Medicinal Chemistry 2015; 22 (24) . https://dx.doi.org/10.2174/0929867322666150619104007
DOI https://dx.doi.org/10.2174/0929867322666150619104007 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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