Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA.
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 1000050, China.
Molecules. 2019 Jan 25;24(3):433. doi: 10.3390/molecules24030433.
has recently surpassed HIV/AIDS as the leading cause of death by a single infectious agent. The standard therapeutic regimen against tuberculosis (TB) remains a long, expensive process involving a multidrug regimen, and the prominence of multidrug-resistant (MDR), extensively drug-resistant (XDR), and totally drug-resistant (TDR) strains continues to impede treatment success. An underexplored class of natural products-the capuramycin-type nucleoside antibiotics-have been shown to have potent anti-TB activity by inhibiting bacterial translocase I, a ubiquitous and essential enzyme that functions in peptidoglycan biosynthesis. The present review discusses current literature concerning the biosynthesis and chemical synthesis of capuramycin and analogs, seeking to highlight the potential of the capuramycin scaffold as a favorable anti-TB therapeutic that warrants further development.
结核病已成为单一传染因子导致死亡的首要原因,超过了艾滋病。抗结核的标准治疗方案仍是一个漫长而昂贵的过程,涉及多种药物治疗,而耐多药(MDR)、广泛耐药(XDR)和完全耐药(TDR)菌株的突出存在继续阻碍治疗的成功。天然产物中一个尚未充分探索的类别——卡泊霉素型核苷抗生素,通过抑制细菌易位酶 I 显示出很强的抗结核活性,易位酶 I 是一种普遍存在且必需的酶,参与肽聚糖生物合成。本文综述了卡泊霉素及其类似物的生物合成和化学合成的最新文献,旨在强调卡泊霉素骨架作为一种有前途的抗结核治疗药物具有进一步开发的潜力。