Total Synthesis of Dragmacidins G and H

被引:1
|
作者
Yamazaki, Keita [1 ]
Okuda, Yuma [1 ]
Takaya, Akiko [1 ]
Nemoto, Tetsuhiro [1 ]
机构
[1] Chiba Univ, Grad Sch Pharmaceut Sci, Chiba 2608675, Japan
关键词
ASYMMETRIC TOTAL-SYNTHESIS; 1ST TOTAL-SYNTHESIS; SPONGE; (+/-)-DRAGMACIDIN; ELUCIDATION;
D O I
10.1021/acs.orglett.3c04039
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The total synthesis of dragmacidins G and H was achieved for the first time by employing nucleophilic aromatic substitution and site-selective cross-coupling reactions using appropriately functionalized pyrazines as substrates. The evaluation of antibacterial activities of dragmacidin G, dragmacidin H, and synthetic analogues against Staphylococcus aureus and the efflux pump-deficient Salmonella Typhimurium revealed that the presence of a Br group on the indole ring adjacent to the sulfide unit was important for increasing antibacterial activities.
引用
收藏
页码:670 / 675
页数:6
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