Benzofuran and benzofuran coumarin derivatives and preparation method and application thereof

The invention discloses benzofuran and coumestans derivatives as shown in formulae (I|), (II) and (III) and a preparation method and an application thereof in treating multidrug-resistant tuberculosis. The benzofuran and coumestans derivatives are anti-mycobacterium tuberculosis compounds which are...

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Hauptverfasser: DONGHAO SHEN, JIE TANG, SHUHUAN WANG, LINGLING LIU, ABIGAIL.L.MANSON, WILLIAM BISHAI, HENDRA GUNOSEWOYO, LIFANG YU, WEI ZHANG, SHICHUN LUN, FAN YANG, ASHLEE.M.EARL
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses benzofuran and coumestans derivatives as shown in formulae (I|), (II) and (III) and a preparation method and an application thereof in treating multidrug-resistant tuberculosis. The benzofuran and coumestans derivatives are anti-mycobacterium tuberculosis compounds which are novel in structure and obvious in antibacterial effect. The compounds taking polyketone synthase coded by a mycobacterium tuberculosis pks13 gene fragment as an acting target spot inhibits growth and reproduction of microorganisms, in particular synthesis of mycolic acid in mycobacterium tuberculosis cell walls. The derivatives have a potential application prospect in the medical field. 本发明公开了如式(I)、(II)、(III)、(IV)所示的苯并呋喃类及Coumestans衍生物及其制备方法,以及所述苯并呋喃类及Coumestans衍生物化合物在治疗耐多药性肺结核疾病中的应用。本发明所述苯并呋喃类及Coumestans衍生物是一类结构新颖,抑菌效果显著的抗结核杆菌化合物,它是以结核杆菌pks13基因片段编码的聚酮合酶为作用靶点,抑制微生物的生长繁殖,尤其是抑制结核分枝杆菌细胞壁中分枝菌酸的合成,在医药领域具有潜在的应用前景。