Literature DB >> 15771435

Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.

Jan Heeres1, Marc R de Jonge, Lucien M H Koymans, Frits F D Daeyaert, Maarten Vinkers, Koen J A Van Aken, Eddy Arnold, Kalyan Das, Amuri Kilonda, Georges J Hoornaert, Frans Compernolle, Marek Cegla, Rasha A Azzam, Koen Andries, Marie-Pierre de Béthune, Hilde Azijn, Rudi Pauwels, Paul J Lewi, Paul A J Janssen.   

Abstract

A series of novel pyrazinones designed as non-nucleoside reverse transcriptase inhibitors (NNRTIs) was synthesized and their anti-HIV structure-activity relationship (SAR) was studied.

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Year:  2005        PMID: 15771435     DOI: 10.1021/jm040829e

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


  6 in total

1.  Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.

Authors:  Bingjie Qin; Xingkai Jiang; Hong Lu; Xingtao Tian; Florent Barbault; Li Huang; Keduo Qian; Chin-Ho Chen; Rong Huang; Shibo Jiang; Kuo-Hsiung Lee; Lan Xie
Journal:  J Med Chem       Date:  2010-07-08       Impact factor: 7.446

2.  From docking false-positive to active anti-HIV agent.

Authors:  Gabriela Barreiro; Joseph T Kim; Cristiano R W Guimarães; Christopher M Bailey; Robert A Domaoal; Ligong Wang; Karen S Anderson; William L Jorgensen
Journal:  J Med Chem       Date:  2007-10-06       Impact factor: 7.446

3.  Tetrasubstituted pyrazinones derived from the reaction of praziquantel with N-bromosuccinimide.

Authors:  Qingjie Zhao; Chunkai Wang; Edward L Ezell; Yuxiang Dong; Jonathan L Vennerstrom
Journal:  Tetrahedron Lett       Date:  2014-08-06       Impact factor: 2.415

4.  Large scale affinity calculations of cyclodextrin host-guest complexes: Understanding the role of reorganization in the molecular recognition process.

Authors:  Lauren Wickstrom; Peng He; Emilio Gallicchio; Ronald M Levy
Journal:  J Chem Theory Comput       Date:  2013-07-09       Impact factor: 6.006

5.  Parameterization of an effective potential for protein-ligand binding from host-guest affinity data.

Authors:  Lauren Wickstrom; Nanjie Deng; Peng He; Ahmet Mentes; Crystal Nguyen; Michael K Gilson; Tom Kurtzman; Emilio Gallicchio; Ronald M Levy
Journal:  J Mol Recognit       Date:  2015-08-10       Impact factor: 2.137

6.  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

  6 in total

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