School of Pharmacy, College of Pharmacy , Taipei Medical University , 250 Wuxing Street , Taipei 11031 , Taiwan .
J Med Chem. 2019 Mar 28;62(6):2851-2893. doi: 10.1021/acs.jmedchem.8b00147. Epub 2018 Nov 1.
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.
硝基被认为是药物化学中一种通用且独特的官能团。尽管硝基在治疗中有很长的应用历史，但它存在毒性问题，通常被归类为结构警示基团或毒性基团，并且与含硝基基团的药物相关的证据存在很大的争议。一般来说，含硝基基团的药物与致突变性和遗传毒性密切相关。在这种情况下，人们已经在努力研究含硝基基团的药物的结构-致突变性或结构-遗传毒性关系。本综述涵盖了含硝基基团的药物的各个方面，包括它们的生物还原激活机制、毒性以及对抗毒性问题的方法。此外，还涵盖了含硝基基团的抗癌、抗结核和抗寄生虫药物领域的最新进展，以及含硝基基团的缺氧激活前药的专利调查。
