Attachment of a 5-nitrofuroyl moiety to spirocyclic piperidines produces non-toxic nitrofurans that are efficacious in vitro against multidrug-resistant Mycobacterium tuberculosis

Mikhail Krasavin, Alexei Lukin, Tatiana Vedekhina, Olga Manicheva, Marine Dogonadze, Tatiana Vinogradova, Natalia Zabolotnykh, Elizaveta Rogacheva, Liudmila Kraeva, Vladimir Sharoyko, Tatiana B. Tennikova, Dmitry Dar'in, Evgeny Sokolovich

Research outputpeer-review

6 Citations (Scopus)

Abstract

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
Publication statusPublished - 15 Mar 2019

Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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