Azaindole Hydroxamic Acids are Potent HIV-1 Integrase Inhibitors

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• 作者：Michael B. Plewe ; Scott L. Butler ; Klaus R. Dress ; Qiyue Hu ; Ted W. Johnson ; Jon E. Kuehler ; Atsuo Kuki ; Hieu Lam ; Wen Liu ; Dawn Nowlin ; Qinghai Peng ; Sadayappan V. Rahavendran ; Steven P. Tanis ; Khanh
• 刊名：Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：November 26, 2009
• 年：2009
• 卷：52
• 期：22
• 页码：7211-7219
• 全文大小：837K
• 年卷期：v.52,no.22(November 26, 2009)
• ISSN：1520-4804

文摘

HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential for viral replication. Recently, HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Herein, we report the discovery of azaindole carboxylic acids and azaindole hydroxamic acids as potent inhibitors of the HIV-1 IN enzyme and their structure−activity relationships. Several 4-fluorobenzyl substituted azaindole hydroxamic acids showed potent antiviral activities in cell-based assays and offered a structurally simple scaffold for the development of novel HIV-1 IN inhibitors.