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 towards 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, and 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.
Original languageEnglish
Pages (from-to)2851-2893
Number of pages43
JournalJournal of Medicinal Chemistry
Issue number6
Publication statusPublished - Mar 28 2019

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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