Synthesis and Preliminary Screening of O-β-D-Galactopyranosides as Potential Mimic of UDP-Galp against Mycobacterium tuberculosis

Synthesis and Preliminary Screening of O-β-D-Galactopyranosides as Potential Mimic of UDP-Galp against Mycobacterium tuberculosis
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DOI:
10.1080/07328303.2011.654017
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发表时间:
2012-01-01
影响因子:
1
通讯作者:
Kartha, K. P. Ravindranathan
Kartha, K. P. Ravindranathan
中科院分区:
化学4区
文献类型:
--
作者:
Mugunthan, G.;Sriram, Dharmarajan;Kartha, K. P. Ravindranathan

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O-吡喃半乳糖苷被合成为尿苷5c-二磷酸吡喃半乳糖(UDP-Galp)的潜在模拟物,UDP-Galp是通过将UDP-Galp转化为UDP-Galf而参与分枝杆菌细胞壁生物合成的β-内酰胺酶的底物。针对结核分枝杆菌H37 Rv菌株的体外测定给出了有希望的结果,最小抑制浓度(MIC)值在3.13至25 μ g/mL的范围内。
O-Galactopyranosides were synthesized as potential mimics of uridine 5c-diphosphate galactopyranose (UDP-Galp), which is the substrate of the mutase enzyme involved in the mycobacterial cell wall biosynthesis by converting UDP-Galp to UDP-Galf. In vitro assay against the Mycobacterium tuberculosis H37Rv strain gave promising results with minimum inhibitory concentration (MIC) values in the range of 3.13 to 25 mu g/mL.