Azaindole Hydroxamic Acids are Potent HIV-1 Integrase Inhibitors
Journal of Medicinal Chemistry2009Vol. 52(22), pp. 7211–7219
Citations Over TimeTop 15% of 2009 papers
Michael Plewe, Scott L. Butler, Klaus Dress, Qiyue Hu, Ted W. Johnson, Jon Kuehler, Atsuo Kuki, Hieu Lam, Wen Liu, Dawn Nowlin, Qinghai Peng, Sadayappan V. Rahavendran, Steven P. Tanis, Khanh Tran, Hai Wang, Anle Yang, Junhu Zhang
Abstract
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.
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