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取代 DXR 抑制剂 FR900098 的膦酸和羟肟酸官能团：提高对结核分枝杆菌活性的尝试。

Substitution of the phosphonic acid and hydroxamic acid functionalities of the DXR inhibitor FR900098: an attempt to improve the activity against Mycobacterium tuberculosis.

机构信息

Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, Biomedical Center, Box 574, SE-751 23 Uppsala, Sweden.

出版信息

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5403-7. doi: 10.1016/j.bmcl.2011.07.005. Epub 2011 Jul 20.

DOI:10.1016/j.bmcl.2011.07.005
PMID:21824775
Abstract

Two series of FR900098/fosmidomycin analogs were synthesized and evaluated for MtDXR inhibition and Mycobacterium tuberculosis whole-cell activity. The design rationale of these compounds involved the exchange of either the phosphonic acid or the hydroxamic acid part for alternative acidic and metal-coordinating functionalities. The best inhibitors provided IC(50) values in the micromolar range, with a best value of 41 μM.

摘要

合成了两个 FR900098/福米霉素类似物系列，并对其进行了 MtDXR 抑制和结核分枝杆菌全细胞活性评价。这些化合物的设计原理包括用替代的酸性和金属配位官能团替换膦酸或羟肟酸部分。最好的抑制剂提供了微摩尔范围内的 IC50 值，最佳值为 41 μM。

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