- The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations
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Using a combination of traditional Medicinal Chemistry/SAR analysis, crystallography, and molecular modeling, we have designed and synthesized a series of novel, highly potent NNRTIs that possess broad antiviral activity against a number of key clinical mutations.
- Tucker, Thomas J.,Saggar, Sandeep,Sisko, John T.,Tynebor, Robert M.,Williams, Theresa M.,Felock, Peter J.,Flynn, Jessica A.,Lai, Ming-Tain,Liang, Yuexia,McGaughey, Georgia,Liu, Meiquing,Miller, Mike,Moyer, Gregory,Munshi, Vandna,Perlow-Poehnelt, Rebecca,Prasad, Sridhar,Sanchez, Rosa,Torrent, Maricel,Vacca, Joseph P.,Wan, Bang-Lin,Yan, Youwei
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- HIV reverse transcriptase inhibitors
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Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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(2010/11/25)
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