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Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: Aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif |
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| Authors: | Dai-Shi Su John J. Lim Elizabeth Tinney Thomas J. Tucker Sandeep Saggar John T. Sisko Bang-Lin Wan Mary Beth Young Kenneth D. Anderson Deanne Rudd Vandna Munshi Carolyn Bahnck Peter J. Felock Meiquing Lu Ming-Tain Lai Sinoeun Touch Gregory Moyer Daniel J. DiStefano Jessica A. Flynn Yuexia Liang Neville J. Anthony |
| Affiliation: | 1. Department of Medicinal Chemistry and Structural Biology, Merck Research Laboratory, PO Box 4, West Point, PA 19486, United States;2. Antiviral Research, Merck Research Laboratory, PO Box 4, West Point, PA 19486, United States;3. Vaccines and Biologics Research, Merck Research Laboratory, PO Box 4, West Point, PA 19486, United States;4. Drug Metabolism, Merck Research Laboratory, PO Box 4, West Point, PA 19486, United States |
| Abstract: | Biaryl ethers were recently reported as potent NNRTIs. Herein, we disclose a detailed effort to modify the previously reported compound 1. We have designed and synthesized a series of novel pyrazole derivatives as a surrogate for pyrazolopyridine motif that were potent inhibitors of HIV-1 RT with nanomolar intrinsic activity on the WT and key mutant enzymes and potent antiviral activity in infected cells. |
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