A selectively antimycobacterial compound belonging to the nitrofuran class of antimicrobials has been developed via conjugation of the nitrofuran moiety to a series of spirocyclic piperidines through an amide linkage. It proved to have comparable activity against drug-sensitive (H37Rv) strain as well as multidrug-resistant, patient-derived strains of Mycobacterium tuberculosis. The compound is druglike, showed no appreciable cytotoxicity toward human retinal pigment epithelial cell line ARPE-19 in concentrations up to 100 μM and displayed low toxicity when evaluated in mice.

Original languageEnglish
Pages (from-to)125-135
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume166
DOIs
StatePublished - 15 Mar 2019

    Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

    Research areas

  • Acylation, Antimycobacterial, ARPE-19 cell line, ESKAPE panel, Multidrug resistance, Nitrofuran antimicrobials, Non-specific toxicity, Periphery optimization, Prins reaction, Spirocycles, Tuberculosis

ID: 39059313