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Publication Abstract from PubMed

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.

Substituted tetrahydroquinolines as potent allosteric inhibitors of reverse transcriptase and its key mutants.,Su DS, Lim JJ, Tinney E, Wan BL, Young MB, Anderson KD, Rudd D, Munshi V, Bahnck C, Felock PJ, Lu M, Lai MT, Touch S, Moyer G, Distefano DJ, Flynn JA, Liang Y, Sanchez R, Prasad S, Yan Y, Perlow-Poehnelt R, Torrent M, Miller M, Vacca JP, Williams TM, Anthony NJ Bioorg Med Chem Lett. 2009 Sep 1;19(17):5119-23. Epub 2009 Jul 10. PMID:19631528^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.