1293387-89-9Relevant academic research and scientific papers
Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors
Johnson, Ted W.,Tanis, Steven P.,Butler, Scott L.,Dalvie, Deepak,Delisle, Dorothy M.,Dress, Klaus R.,Flahive, Erik J.,Hu, Qiyue,Kuehler, Jon E.,Kuki, Atsuo,Liu, Wen,McClellan, Guy A.,Peng, Qinghai,Plewe, Michael B.,Richardson, Paul F.,Smith, Graham L.,Solowiej, Jim,Tran, Khanh T.,Wang, Hai,Yu, Xiaoming,Zhang, Junhu,Zhu, Huichun
, p. 3393 - 3417 (2011/07/08)
Figure Presented. HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential for viral replication, and HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Recently, we reported the synthesis of orally bioavailable azaindole hydroxamic acids that were potent inhibitors of the HIV-1 IN enzyme. Here we disclose the design and synthesis of novel tricyclic N-hydroxy-dihydronaphthyridinones as potent, orally bioavailable HIV-1 integrase inhibitors displaying excellent ligand and lipophilic efficiencies.
