Institute of Chemistry, St. Petersburg State University, St. Petersburg, Russian Federation.
Curr Med Chem. 2021;28(29):5926-5982. doi: 10.2174/0929867328666210216114838.
The last decade has been characterized by the development and approval of pretomanid and delamanid, which are nitroimidazole based drugs for multidrug -resistant tuberculosis. This attracted renewed attention to the nitroheterocyclic scaffolds as a source of safe and efficient antimicrobial agents. While the primary focus is still on nitrofurans and nitroimidazoles, well known as bioreducible prodrugs, a number of studies have been published on other 5-membered nitroheteroaromatic compounds. The latter not only show promising antimicrobial activity but also demonstrate modes of action different from the conventional reductive activation of the nitro group. Considering the potential of these efforts to impact the continuing race against drug-resistant pathogens, herein we review non-furan/imidazole-based 5-membered nitroheteroaromatics investigated as antimicrobial agents in 2010-2020.
过去十年的特点是开发和批准了丙硫异烟胺和德拉马尼,这两种药物都是基于硝基咪唑的抗多重耐药结核药物。这再次引起了人们对硝基杂环支架作为安全有效的抗菌药物来源的关注。虽然重点仍然是硝基呋喃和硝基咪唑,它们是众所周知的生物还原前药,但已经发表了许多关于其他 5 元硝基杂芳族化合物的研究。后者不仅显示出有希望的抗菌活性,而且表现出与传统的硝基还原激活不同的作用模式。考虑到这些努力对抗耐药病原体的持续竞赛的潜力,本文综述了 2010 年至 2020 年作为抗菌药物研究的非呋喃/咪唑基 5 元硝基杂芳族化合物。