Inhibitors of HIV-1 attachment. Part 3: A preliminary survey of the effect of structural variation of the benzamide moiety on antiviral activity

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• 作者：Nicholas A. Meanwell ; Owen B. Wallace ; Henry Wang ; Milind Deshp ; e ; Bradley C. Pearce ; Ashok Trehan ; Kap-Sun Yeung ; Zhilei Qiu ; J.J. Kim Wright ; Brett A. Robinson ; Yi-Fei Gong ; Hwei-Gene Heidi Wang ; Wa
• 关键词：HIV attachment inhibitor ; Antiviral ; Indole glyoxamide ; HIV inhibitor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：1 September 2009
• 年：2009
• 卷：19
• 期：17
• 页码：5136-5139
• 全文大小：239 K

文摘

1-(4-Benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione (1a) has been characterized as an inhibitor of HIV-1 attachment that interferes with the interaction of viral gp120 with the host cell receptor CD4. In previous studies, the effect of indole substitution pattern on antiviral activity was probed. In this Letter, the effect of structural variation of the benzamide moiety is described, a study that reveals the potential or the phenyl moiety to be replaced by five-membered heterocyclic rings and a restricted tolerance for the introduction of substituents to the phenyl ring.