Literature DB >> 16503141

Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant.

Ester Muraglia1, Olaf D Kinzel, Ralph Laufer, Michael D Miller, Gregory Moyer, Vandna Munshi, Federica Orvieto, Maria Cecilia Palumbi, Giovanna Pescatore, Michael Rowley, Peter D Williams, Vincenzo Summa.   

Abstract

A series of aryltetrazolylacetanilides was synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors on wild-type virus and on the clinically relevant K103N mutant strain. Extensive SAR investigation led to potent compounds, with nanomolar activity on K103N, and orally bioavailable in rats.

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Year:  2006        PMID: 16503141     DOI: 10.1016/j.bmcl.2006.02.024

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  9 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.  Synthesis of peptidomimetics, δ- and ε-lactam tetrazoles.

Authors:  Steven Gunawan; Kristen Keck; Alex Laetsch; Christopher Hulme
Journal:  Mol Divers       Date:  2012-05-24       Impact factor: 2.943

3.  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

4.  Search for non-nucleoside inhibitors of HIV-1 reverse transcriptase using chemical similarity, molecular docking, and MM-GB/SA scoring.

Authors:  Gabriela Barreiro; Cristiano R W Guimarães; Ivan Tubert-Brohman; Theresa M Lyons; Julian Tirado-Rives; William L Jorgensen
Journal:  J Chem Inf Model       Date:  2007-10-20       Impact factor: 4.956

Review 5.  Tetrazoles via Multicomponent Reactions.

Authors:  Constantinos G Neochoritis; Ting Zhao; Alexander Dömling
Journal:  Chem Rev       Date:  2019-02-01       Impact factor: 60.622

6.  2-(1,3-Dioxoisoindolin-2-yl)acetonitrile.

Authors:  Younas Aouine; Anouar Alami; Abdelilah El Hallaoui; Abdelrhani Elachqar; Hafid Zouihri
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-09-25

7.  Selective anticancer activities of ruthenium(II)-tetrazole complexes and their mechanistic insights.

Authors:  Chanchal Sonkar; Novina Malviya; Nilima Sinha; Attreyee Mukherjee; Srimanta Pakhira; Suman Mukhopadhyay
Journal:  Biometals       Date:  2021-04-26       Impact factor: 2.949

Review 8.  Isocyanide-based multicomponent reactions towards cyclic constrained peptidomimetics.

Authors:  Gijs Koopmanschap; Eelco Ruijter; Romano Va Orru
Journal:  Beilstein J Org Chem       Date:  2014-03-04       Impact factor: 2.883

Review 9.  Approved HIV reverse transcriptase inhibitors in the past decade.

Authors:  Guangdi Li; Yali Wang; Erik De Clercq
Journal:  Acta Pharm Sin B       Date:  2021-11-16       Impact factor: 14.903

  9 in total

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