Library of 1,4-disubstituted 1,2,3-triazole analogs of oxazolidinone RNA-binding agents.
Library of 1,4-disubstituted 1,2,3-triazole analogs of oxazolidinone RNA-binding agents.
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DOI：
10.1021/cc100029y
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发表时间：
2010-07-12
影响因子：
--
通讯作者：
Bergmeier SC
中科院分区：
文献类型：
--
作者：
Acquaah-Harrison G;Zhou S;Hines JV;Bergmeier SC
靶向 RNA 的小分子的设计和合成在抗菌治疗中非常重要。我们之前报道过一系列 4,5-二取代 2-恶唑烷酮的 RNA 结合，这些化合物与细菌 RNA 高度保守的凸起区域结合。这种生物靶标T盒抗终止系统主要存在于革兰氏阳性菌中，调节多种氨基酸相关基因的表达。为了扩大我们的文库，我们制备了一个 1,4-二取代 1,2,3-三唑类似物文库，它需要等排取代恶唑烷酮核。通过叠氮化物和炔环加成反应的铜(I)催化增强了新类似物的合成。共制备了108种1,4-二取代1,2,3-三唑化合物。所有化合物均作为 RNA 结合剂进行评估。
The design and synthesis of small molecules that target RNA is immensely important in antibacterial therapy. We had previously reported on the RNA binding of a series of 4,5-disubstituted 2-oxazolidinones that bind to a highly conserved bulge region of bacterial RNA. This biological target T box antitermination system, which is found mainly in Gram-positive bacteria, regulates the expression of several amino acid related genes. In an effort to amplify our library, we have prepared a library of 1,4-disubstituted 1,2,3-triazole analogs that entails an isosteric replacement of the oxazolidinone nucleus. The synthesis of the new analogs was enhanced via copper(I) catalysis of an azide and alkyne cycloaddition reaction. A total of 108 1,4-disubstituted 1,2,3-triazole compounds have been prepared. All compounds were evaluated as RNA binding agents.
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影响因子：
5.2
作者：
Sabitha, G;Babu, RS;Yadav, JS
通讯作者：
Yadav, JS
影响因子：
3.2
作者：
GRUNDY, FJ;ROLLINS, SM;HENKIN, TM
通讯作者：
HENKIN, TM
影响因子：
3.6
作者：
ONAKA, M;SUGITA, K;IZUMI, Y
通讯作者：
IZUMI, Y
影响因子：
1.8
作者：
Collin, Marie-Pierre;Hobbie, Sven N.;Vasella, Andrea
通讯作者：
Vasella, Andrea
影响因子：
2.7
作者：
Means, JA;Hines, JV
通讯作者：
Hines, JV