期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 6, 页码 2758-2768出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm201694y
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资金
- CNRS
- Crunch (Interregional Organic Chemistry Network)
The synthesis of new class of potential TPase inhibitors containing a difluoromethylphosphonate function as phosphate mimic is reported. This new series was prepared from a readily available fluorinated building block in few steps. Two series were evaluated as potential inhibitors: a linear series and a conformational constrained series. The activity of these multisubstrate inhibitors depends on the size of the spacer introduced between the pyrimidine ring and the phosphonate function. Best results were observed from triazolyl derivatives, easily obtained from propargylthymine and corresponding azides.
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