Literature DB >> 15771449

Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.

Jerome Guillemont1, Elisabeth Pasquier, Patrice Palandjian, Daniel Vernier, Sandrine Gaurrand, Paul J Lewi, Jan Heeres, Marc R de Jonge, Lucien M H Koymans, Frits F D Daeyaert, Maarten H Vinkers, Eddy Arnold, Kalyan Das, Rudi Pauwels, Koen Andries, Marie-Pierre de Béthune, Eva Bettens, Kurt Hertogs, Piet Wigerinck, Philip Timmerman, Paul A J Janssen.   

Abstract

This paper reports the synthesis and the antiviral properties of new diarylpyrimidine (DAPY) compounds as nonnucleoside reverse transcriptase inhibitors (NNRTIs). The synthesis program around this new DAPY series was further optimized to produce compounds displaying improved activity against a panel of eight clinically relevant single and double mutant strains of human immunodeficiency virus type 1 (HIV-1).

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Year:  2005        PMID: 15771449     DOI: 10.1021/jm040838n

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


  13 in total

1.  The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.

Authors:  Vigneshwaran Namasivayam; Murugesan Vanangamudi; Victor G Kramer; Sonali Kurup; Peng Zhan; Xinyong Liu; Jacob Kongsted; Siddappa N Byrareddy
Journal:  J Med Chem       Date:  2018-12-27       Impact factor: 7.446

2.  2D and 3D QSAR studies of diarylpyrimidine HIV-1 reverse transcriptase inhibitors.

Authors:  Joseph Rebehmed; Florent Barbault; Cátia Teixeira; François Maurel
Journal:  J Comput Aided Mol Des       Date:  2008-05-28       Impact factor: 3.686

3.  Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.

Authors:  Na Liu; Bingjie Qin; Lian-Qi Sun; Fei Yu; Lu Lu; Shibo Jiang; Kuo-Hsiung Lee; Lan Xie
Journal:  Bioorg Med Chem Lett       Date:  2014-07-11       Impact factor: 2.823

4.  HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site.

Authors:  Daniel M Himmel; Stefan G Sarafianos; Sanjeewa Dharmasena; Mohammed M Hossain; Kessler McCoy-Simandle; Tatiana Ilina; Arthur D Clark; Jennifer L Knight; John G Julias; Patrick K Clark; Karsten Krogh-Jespersen; Ronald M Levy; Stephen H Hughes; Michael A Parniak; Eddy Arnold
Journal:  ACS Chem Biol       Date:  2006-12-20       Impact factor: 5.100

5.  Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.

Authors:  Xingtao Tian; Bingjie Qin; Hong Lu; Weihong Lai; Shibo Jiang; Kuo-Hsiung Lee; Chin Ho Chen; Lan Xie
Journal:  Bioorg Med Chem Lett       Date:  2009-07-19       Impact factor: 2.823

6.  High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations.

Authors:  Kalyan Das; Joseph D Bauman; Arthur D Clark; Yulia V Frenkel; Paul J Lewi; Aaron J Shatkin; Stephen H Hughes; Eddy Arnold
Journal:  Proc Natl Acad Sci U S A       Date:  2008-01-29       Impact factor: 11.205

7.  Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.

Authors:  Mariela Bollini; José A Cisneros; Krasimir A Spasov; Karen S Anderson; William L Jorgensen
Journal:  Bioorg Med Chem Lett       Date:  2013-07-08       Impact factor: 2.823

8.  Biochemical mechanism of HIV-1 resistance to rilpivirine.

Authors:  Kamalendra Singh; Bruno Marchand; Devendra K Rai; Bechan Sharma; Eleftherios Michailidis; Emily M Ryan; Kayla B Matzek; Maxwell D Leslie; Ariel N Hagedorn; Zhe Li; Pieter R Norden; Atsuko Hachiya; Michael A Parniak; Hong-Tao Xu; Mark A Wainberg; Stefan G Sarafianos
Journal:  J Biol Chem       Date:  2012-09-06       Impact factor: 5.157

9.  Switch to Rilpivirine/Emtricitabine/Tenofovir Single-Tablet Regimen of Human Immunodeficiency Virus-1 RNA-Suppressed Patients, Agence Nationale de Recherches sur le SIDA et les Hépatites Virales CO3 Aquitaine Cohort, 2012-2014.

Authors:  Charles Cazanave; Sandrine Reigadas; Cyril Mazubert; Pantxika Bellecave; Mojgan Hessamfar; Fabien Le Marec; Estibaliz Lazaro; Gilles Peytavin; Mathias Bruyand; Hervé Fleury; François Dabis; Didier Neau
Journal:  Open Forum Infect Dis       Date:  2015-03-12       Impact factor: 3.835

10.  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

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