A novel diketo phosphonic acid that exhibits specific, strand-transfer inhibition of HIV integrase and anti-HIV activity
A novel diketo phosphonic acid that exhibits specific, strand-transfer inhibition of HIV integrase and anti-HIV activity
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DOI：
10.1016/j.bmcl.2006.12.009
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发表时间：
2007-03-01
影响因子：
2.7
通讯作者：
Pommier, Yves
中科院分区：
文献类型：
--
作者：
Chi, Guochen;Nair, Vasu;Pommier, Yves
我们合成了新型磷酸二酮酸类似物。有趣的是，我们的抗hiv化合物1的磷酸异戊二酯2，仅是链转移步骤的抑制剂，与1形成鲜明对比。化合物2的抗hiv活性低于1，但比膦酸类似物L-708906的活性更强，毒性更小。这些同构化合物代表了具有结构、合成和抗病毒兴趣的β -二酮膦酸的第一个例子。(c) 2006 Elsevier Ltd.版权所有。
We have synthesized novel phosphonic acid analogues of P-diketo acids. Interestingly, the phosphonic acid isostere, 2, of our anti-HIV compound, 1, was an inhibitor of only the strand transfer step, in stark contrast to 1. Compound 2 had lower anti-HIV activity than 1, but was more active and less toxic than the phosphonic acid analogue of L-708906. These isosteric compounds represent the first examples of beta-diketo phosphonic acids of structural, synthetic, and antiviral interest. (c) 2006 Elsevier Ltd. All rights reserved.