化学
硝基
前药
背景(考古学)
硝基化合物
遗传毒性
药理学
毒性
立体化学
有机化学
生物化学
医学
生物
烷基
古生物学
作者
Kunal Nepali,Hsueh‐Yun Lee,Jing‐Ping Liou
标识
DOI:10.1021/acs.jmedchem.8b00147
摘要
The nitro group is considered to be a versatile and unique functional group in medicinal chemistry. Despite a long history of use in therapeutics, the nitro group has toxicity issues and is often categorized as a structural alert or a toxicophore, and evidence related to drugs containing nitro groups is rather contradictory. In general, drugs containing nitro groups have been extensively associated with mutagenicity and genotoxicity. In this context, efforts toward the structure–mutagenicity or structure–genotoxicity relationships have been undertaken. The current Perspective covers various aspects of agents that contain nitro groups, their bioreductive activation mechanisms, their toxicities, and approaches to combat their toxicity issues. In addition, recent advances in the field of anticancer, antitubercular and antiparasitic agents containing nitro groups, along with a patent survey on hypoxia-activated prodrugs containing nitro groups, are also covered.
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