AI Article Synopsis
- Structure modification of drugs, particularly late-stage functionalization (LSF), is effective for optimizing lead compounds, and this study focused on Cu-catalyzed C-H LSF of 5-nitrofuran drugs.
- Multiple modifications were performed on the 5-nitrofuran drugs, including hydroxylation, methylation, azidination, cyanation, and arylation, and the antibacterial activities of the new compounds were tested.
- Among the modified compounds, compounds 1 and 18 showed the highest antibacterial activity, while cell cytotoxicity assays were conducted on potent compounds and the parent drug to assess safety.
Article 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, Antibacterial activities of all compounds 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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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9853512 | PMC |
| http://dx.doi.org/10.1039/d2ra07676d | DOI Listing |
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