Late-stage functionalization of 5-nitrofurans derivatives and their antibacterial activities?
RSC Advances Pub Date: 2023-01-20 DOI: 10.1039/D2RA07676D
Abstract
Structure modification of drugs is a reliable way to optimize lead compounds, among which the most striking and direct method is late-stage functionalization (LSF). Here, we employed the Cu-catalyzed C–H LSF to modify 5-nitrofuran drugs. A series of modifications have been carried out including hydroxylation, methylation, azidination, cyanation, arylation, etc. Antibacterial activities of all compounds in vitro were measured. The results showed that compound 1 and compound 18 were the most active among all compounds. Meanwhile, the cell cytotoxicity assays of potent compounds 1, 3, 4, 5 & 18 and the parent drug FZD were conducted.
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Journal Name：RSC Advances
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CAS no.: 89640-58-4
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