期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 166, 期 -, 页码 125-135出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.01.050
关键词
Tuberculosis; Multidrug resistance; Antimycobacterial; Nitrofuran antimicrobials; Periphery optimization; Non-specific toxicity; Spirocycles; Prins reaction; Acylation; ESKAPE panel; ARPE-19 cell line
资金
- Russian Scientific Fund [14-50-00069]
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 mu M and displayed low toxicity when evaluated in mice. (C) 2019 Elsevier Masson SAS. All rights reserved.
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