Structure–activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity

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• 作者：Abdellah Benjahad ; Said Oumouch ; Jer&#xf4 ; me Guillemont ; Elisabeth Pasquier ; Dominique Mabire ; Koen Andries ; Chi Hung Nguyen ; David S. Grierson
• 关键词：NNRTI ; Pyridinone ; IOPY ; Anti-HIV
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 February 2007
• 卷：17
• 期：3
• 页码：712-716
• 文件大小：188 K

摘要

As part of a systematic SAR study on the 3-iodo-4-phenoxypyridinone 3 (IOPY) type non-nucleoside reverse transcriptase inhibitors, the analogues 4a–4z bearing different C-3 substituents were synthesized and evaluated for their anti-HIV activity against wild-type HIV-1 and four of the principal HIV mutant strains (K103N, Y181C, Y188L, and I100L). The results show that the 3-vinyl analogue 4j is the only compound which displays anti-HIV activity comparable to IOPY 3, and in this respect represents a possible back-up to this lead molecule.