Recent advancement in drug development of nitro(NO₂)‐heterocyclic compounds as lead scaffolds for the treatment of Mycobacterium tuberculosis

Abstract

Tuberculosis (TB) is an infectious disease caused predominantly by Mycobacterium tuberculosis (Mtb). It was responsible for approximately 1.4 million deaths worldwide in 2019. The lack of new drugs to treat drug-resistant strains is a principal factor for the slow rise in TB infections. Our aim is to aid the development of new TB treatments by describing improvements (last decade, 2011-2021) to nitro(NO 2 )-based compounds that have shown activity or pharmacological properties (e.g., anti-proliferative, anti-kinetoplastid) against Mtb. For all compounds, we have included final correlations of minimum inhibitory concentrations against Mtb (H 37 Rv).

Design and Synthesis of Novel 3-Nitro-1H-1,2,4-triazole-1,2,3-triazole-1,4-disubstituted Analogs as Promising Antitrypanosomatid Agents: Evaluation of In Vitro Activity against Chagas Disease and Leishmaniasis

“…Nitroheterocycles are widely used in medicinal chemistry due to their versatile applications, such as analgesics, anti-inflammatories, antimicrobials, antitubercular, antiparasitic, and more (Figure ). − However, nitro groups can also be associated with mutagenic and carcinogenic effects, which can limit their use in drug discovery . Nitrofurans (such as Nifurtimox 2 ) and 5-nitroimidazoles (such as megazole 12 ) are examples of compounds that exhibit such toxicities.…”