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.
Keywords: ARPE-19 cell line; Acylation; Antimycobacterial; ESKAPE panel; Multidrug resistance; Nitrofuran antimicrobials; Non-specific toxicity; Periphery optimization; Prins reaction; Spirocycles; Tuberculosis.
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