Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1363717 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Dai-Shi Su, John J. Lim, Elizabeth Tinney, Bang-Lin Wan, Mary Beth Young, Kenneth D. Anderson, Deanne Rudd, Vandna Munshi, Carolyn Bahnck, Peter J. Felock, Meiqing Lu, Ming-Tain Lai, Sinoeun Touch, Gregory Moyer, Daniel J. DiStefano, Jessica A. Flynn,