Medium-Ring Nitrogen Heterocycles through Migratory Ring Expansion of Metalated Ureas
Simple benzo-fused nitrogen heterocycles (indolines, tetrahydroquinolines, and their homologues) undergo migratory ring expansion through deprotonation of their benzylic urea derivatives with lithium diisopropylamide (LDA) in the presence of N,N′-dimethyl
Hall, Jessica E.,Matlock, Johnathan V.,Ward, John W.,Gray, Katharine V.,Clayden, Jonathan
supporting information
p. 11153 - 11157
(2016/10/13)
Substituted tetrahydroquinolines as potent allosteric inhibitors of reverse transcriptase and its key mutants
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are key elements of multidrug regimens, called HAART (Highly Active Antiretroviral Therapy), that are used to treat HIV-1 infections. Elucidation of the structure-activity relationships of the thiocarbamate moiety of the previous published lead compound 2 provided a series of novel tetrahydroquinoline derivatives as potent inhibitors of HIV-1 RT with nanomolar intrinsic activity on the WT and key mutant enzymes and potent antiviral activity in infected cells. The SAR optimization, mutation profiles, preparation of compounds, and pharmacokinetic profile of compounds are described.
Su, Dai-Shi,Lim, John J.,Tinney, Elizabeth,Wan, Bang-Lin,Young, Mary Beth,Anderson, Kenneth D.,Rudd, Deanne,Munshi, Vandna,Bahnck, Carolyn,Felock, Peter J.,Lu, Meiqing,Lai, Ming-Tain,Touch, Sinoeun,Moyer, Gregory,DiStefano, Daniel J.,Flynn, Jessica A.,Liang, Yuexia,Sanchez, Rosa,Prasad, Sridhar,Yan, Youwei,Perlow-Poehnelt, Rebecca,Torrent, Maricel,Miller, Mike,Vacca, Joe P.,Williams, Theresa M.,Anthony, Neville J.
scheme or table
p. 5119 - 5123
(2010/03/31)
More Articles about upstream products of 103661-43-4