Library of 1,4-Disubstituted 1,2,3-Triazole Analogs of Oxazolidinone RNA-Binding Agents

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• 作者：George Acquaah-Harrison ; Shu Zhou ; Jennifer V. Hines ; Stephen C. Bergmeier
• 刊名：Journal of Combinatorial Chemistry
• 出版年：2010
• 出版时间：July 12, 2010
• 年：2010
• 卷：12
• 期：4
• 页码：491-496
• 全文大小：218K
• 年卷期：v.12,no.4(July 12, 2010)
• ISSN：1520-4774

文摘

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.