同核和异核双靛蓝衍生物的设计、合成及体外抗分枝杆菌活性。
Design, synthesis and in vitro anti-mycobacterial activities of homonuclear and heteronuclear bis-isatin derivatives.
机构信息
State Key Laboratory of Advanced Technology for Materials Synthesis and Processing, Wuhan University of Technology, Wuhan, Hubei, PR China.
State Key Laboratory of Advanced Technology for Materials Synthesis and Processing, Wuhan University of Technology, Wuhan, Hubei, PR China.
出版信息
Fitoterapia. 2018 Jun;127:383-386. doi: 10.1016/j.fitote.2018.03.018. Epub 2018 Apr 6.
A series of novel homonuclear and heteronuclear bis-isatin derivatives tethered through ethylene were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities against MTB H37Rv and MDR-TB. All hybrids exhibited potential anti-mycobacterial activities against MTB H37Rv and MDR-TB with MIC ranging from 16 to 256 μg/mL. In particular, the heteronuclear bis-isatin 4i (MIC: 25 and 16 μg/mL) was most active against MTB H37Rv and MDR-TB strains, and could act as a lead for further optimization.
设计、合成了一系列通过亚乙基连接的新型同核和异核双靛红衍生物，并评估了它们对结核分枝杆菌 H37Rv 和耐多药结核分枝杆菌的体外抗结核活性。所有杂合体对结核分枝杆菌 H37Rv 和耐多药结核分枝杆菌均表现出潜在的抗结核活性，MIC 范围为 16 至 256μg/mL。特别是异核双靛红 4i（MIC：25 和 16μg/mL）对结核分枝杆菌 H37Rv 和耐多药结核分枝杆菌菌株最为活跃，可作为进一步优化的先导化合物。
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