The abyssomicin C family as in vitro inhibitors of Mycobacterium tuberculosis.

The abyssomicin C family as in vitro inhibitors of Mycobacterium tuberculosis.
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DOI:
10.1016/j.tube.2010.08.002
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发表时间:
2010-09
期刊:
Tuberculosis (Edinburgh, Scotland)
影响因子:
--
通讯作者:
Sacchettini JC
Sacchettini JC
中科院分区:
其他
文献类型:
--
作者:
Freundlich JS;Lalgondar M;Wei JR;Swanson S;Sorensen EJ;Rubin EJ;Sacchettini JC

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鉴于有报道称其能抑制枯草芽孢杆菌对氨基苯甲酸酯的生物合成,研究人员对abyssomicin C家族的天然产物以及一种关键的合成中间体的抑菌效果进行了研究。天然存在的(−)-abyssomicin C及其atropisomer对生长相对较快且无毒的耻垢分枝杆菌和牛分枝杆菌BCG疫苗株具有较低的微摩尔生长抑制作用,而它们的对跖体活性略低。(−)-Abyssomicin C及其atropisomer对结核分枝杆菌H37Rv特别有效,MIC值分别为3.6 μM和7.2 μM。更具体地说,(−)-abyssomicin C具有杀菌作用。因此,这种复杂的天然产物及其类似物有望成为研究结核分枝杆菌代谢的化学工具。
The antimycobacterial efficacy of the abyssomicin C family of natural products, in addition to a key synthetic intermediate, has been investigated given their reported inhibition of Bacillus subtilis p-aminobenzoate biosynthesis. The naturally occurring (−)-abyssomicin C and its atropisomer were found to exhibit low micromolar growth inhibition against the relatively fast-growing and non-virulent Mycobacterium smegmatis and the vaccine strain Mycobacterium bovis BCG, while their antipodes were slightly less active. (−)-Abyssomicin C and its atropisomer were particularly efficacious against Mycobacterium tuberculosis H37Rv, exhibiting MIC values of 3.6 and 7.2 μM, respectively. More specifically, (−)-abyssomicin C was bactericidal. This complex natural product and its analogs, thus, hold promise as chemical tools in the study of M. tuberculosis metabolism.
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