Chen Geshuyi, Chang Zhe, Yuan Pei, Wang Si, Yang Yongxiu, Liang Xiaolei, Zhao Depeng
The First Clinical Medical College, Lanzhou University Lanzhou China
Guangdong Provincial Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University Guangzhou China
RSC Adv. 2023 Jan 20;13(5):3204-3209. doi: 10.1039/d2ra07676d. eCollection 2023 Jan 18.
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.
药物的结构修饰是优化先导化合物的可靠方法，其中最显著且直接的方法是后期官能团化（LSF）。在此，我们采用铜催化的C-H后期官能团化来修饰5-硝基呋喃类药物。已进行了一系列修饰，包括羟基化、甲基化、叠氮化、氰化、芳基化，并测定了所有化合物的抗菌活性。结果表明，化合物1和化合物18在所有化合物中活性最高。同时，对活性较强的化合物1、3、4、5和18以及母体药物FZD进行了细胞毒性测定。
