Literature DB >> 19883100

Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.

Dai-Shi Su1, John J Lim, Elizabeth Tinney, 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, Rosa Sanchez, Rebecca Perlow-Poehnelt, Mike Miller, Joe P Vacca, Theresa M Williams, Neville J Anthony.   

Abstract

Biaryl ethers were recently reported as potent NNRTIs. Herein we disclose a detailed SAR study that led to the biaryl ether 6. This compound possessed excellent potency against WT RT and key clinically observed RT mutants and had an excellent pharmacokinetic profile in rats, dogs, and rhesus macaques. The compound also exhibited a clean safety profile in preclinical safety studies.

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Year:  2009        PMID: 19883100     DOI: 10.1021/jm901230r

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  5 in total

1.  Facile synthesis of symmetrical bis(benzhydryl)ethers using p-toluenesulfonyl chloride under solvent-free conditions.

Authors:  Goutam Brahmachari; Bubun Banerjee
Journal:  Org Med Chem Lett       Date:  2013-02-18

Review 2.  Non-nucleoside reverse transcriptase inhibitors: a review on pharmacokinetics, pharmacodynamics, safety and tolerability.

Authors:  Iris Usach; Virginia Melis; José-Esteban Peris
Journal:  J Int AIDS Soc       Date:  2013-09-04       Impact factor: 5.396

3.  Synthesis, Immunosuppressive Properties, and Mechanism of Action of a New Isoxazole Derivative.

Authors:  Marcin Mączyński; Sylwia Borska; Katarzyna Mieszała; Maja Kocięba; Ewa Zaczyńska; Iwona Kochanowska; Michał Zimecki
Journal:  Molecules       Date:  2018-06-26       Impact factor: 4.411

4.  A comparison of the ability of rilpivirine (TMC278) and selected analogues to inhibit clinically relevant HIV-1 reverse transcriptase mutants.

Authors:  Barry C Johnson; Gary T Pauly; Ganesha Rai; Disha Patel; Joseph D Bauman; Heather L Baker; Kalyan Das; Joel P Schneider; David J Maloney; Eddy Arnold; Craig J Thomas; Stephen H Hughes
Journal:  Retrovirology       Date:  2012-12-05       Impact factor: 4.602

5.  N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.

Authors:  Mikhail S Novikov; Vladimir T Valuev-Elliston; Denis A Babkov; Maria P Paramonova; Alexander V Ivanov; Sergey A Gavryushov; Anastasia L Khandazhinskaya; Sergey N Kochetkov; Christophe Pannecouque; Graciela Andrei; Robert Snoeck; Jan Balzarini; Katherine L Seley-Radtke
Journal:  Bioorg Med Chem       Date:  2013-01-03       Impact factor: 3.641

  5 in total

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