posted on 2018-10-08, 00:00authored byKunal Nepali, Hsueh-Yun Lee, Jing-Ping Liou
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.