Article
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
Bioorganic & medicinal chemistry letters - 1 Aug 2010
Su Dai-Shi, Lim John J, Tinney Elizabeth, Tucker Thomas J, Saggar Sandeep, Sisko John T, Wan Bang-Lin, Young Mary Beth, Anderson Kenneth D, Rudd Deanne, Munshi Vandna, Bahnck Carolyn, Felock Peter J, Lu Meiquing, Lai Ming-Tain, Touch Sinoeun, Moyer Gregory, Distefano Daniel J, Flynn Jessica A, Liang Yuexia, Sanchez Rosa, Perlow-Poehnelt Rebecca, Miller Mike, Vacca Joe P, Williams Theresa M, Anthony Neville J
Abstract excerpt
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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