Pyranocoumarin, a novel anti-TB pharmacophore: synthesis and biological evaluation against Mycobacterium tuberculosis.
Pyranocoumarin, a novel anti-TB pharmacophore: synthesis and biological evaluation against Mycobacterium tuberculosis.
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DOI：
10.1016/j.bmc.2006.02.017
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发表时间：
2006-07
影响因子：
3.5
通讯作者：
Ze-Qi Xu;K. Pupek;W. J. Suling;L. Enache;M. Flavin
中科院分区：
文献类型：
--
作者：
Ze-Qi Xu;K. Pupek;W. J. Suling;L. Enache;M. Flavin
吡喃香豆素类化合物被鉴定为具有抗TB活性的新颖且独特的药效团。采用系统的方法来研究结构特征。合成化合物的聚焦文库，并在初步筛选测定中评价其抗TB活性。进一步测定显示有活性的化合物的MIC和MBC值。四种杀菌化合物中的三种（16、17 c和18 f）是氨基衍生物，MIC值为16μg/mL，MBC值分别为32、32和64μg/mL。
Pyranocoumarin compounds were identified to embody a novel and unique pharmacophore for anti-TB activity. A systematic approach was taken to investigate the structural characteristics. Focused libraries of compounds were synthesized and evaluated for their anti-TB activity in primary screening assays. Compounds shown to be active were further determined for MIC and MBC values. Three of the four bactericidal compounds (16, 17c, and 18f) were amino derivatives, with MIC values of 16μg/mL and respective MBC values of 32, 32, and 64μg/mL.