A novel diketo phosphonic acid that exhibits specific, strand-transfer inhibition of HIV integrase and anti-HIV activity

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:17

Article

Chi, Guochen ; Nair, Vasu ; Semenova, Elena ; Pommier, Yves

关键词: synthesis;    phosphonates;    HIV integrase inhibitors;    mechanism of inhibition;    anti-HIV activity;   

DOI  :  10.1016/j.bmcl.2006.12.009

来源: Elsevier

【 摘 要 】

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.

【 授权许可】

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