Search Results - "Coates, Jonathan A. V."
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Small molecule inhibitors of the LEDGF site of human immunodeficiency virus integrase identified by fragment screening and structure based design
Published in PloS one (10-07-2012)“…A fragment-based screen against human immunodeficiency virus type 1 (HIV) integrase led to a number of compounds that bound to the lens epithelium derived…”
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Antiviral agents 3. Discovery of a novel small molecule non-nucleoside inhibitor of Hepatitis B Virus (HBV)
Published in Bioorganic & medicinal chemistry letters (15-03-2011)“…The discovery of a small molecule non-nucleoside inhibitor of Hepatitis B Virus is described. During our work on conocurvone derived naphthoquinone ‘trimers’…”
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Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold
Published in Bioorganic & medicinal chemistry letters (01-10-2010)“…HIV integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization…”
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Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: Azoles: Effective metal chelators
Published in Bioorganic & medicinal chemistry letters (01-10-2010)“…Synthesis of a diverse set of azoles and their utilizations as an amide isostere in the design of HIV integrase inhibitors is described. The Letter identified…”
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Antiviral agents 2. Synthesis of trimeric naphthoquinone analogues of conocurvone and their antiviral evaluation against HIV
Published in Bioorganic & medicinal chemistry (01-09-2010)“…The synthesis of a new series of conocurvone analogues is presented that explores the importance of the pyran rings of conocurvone, their degree of…”
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Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses
Published in Bioorganic & medicinal chemistry letters (01-09-2010)“…A series of novel HIV integrase inhibitors active against rategravir resistant strains are reported. Initial SAR studies revealed that activities against…”
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Crystal Structures of Novel Allosteric Peptide Inhibitors of HIV Integrase Identify New Interactions at the LEDGF Binding Site
Published in Chembiochem : a European journal of chemical biology (17-10-2011)“…An optimised method of solution cyclisation gave us access to a series of peptides including SLKIDNLD (2). We investigated the crystallographic complexes of…”
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Structural Basis for a New Mechanism of Inhibition of H I V-1 Integrase Identified by Fragment Screening and Structure-Based Design
Published in Antiviral chemistry & chemotherapy (01-04-2011)“…Background: HIV-1 integrase is a clinically validated therapeutic target for the treatment of HIV-1 infection, with one approved therapeutic currently on the…”
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Fluoro carbocyclic nucleosides: synthesis and antiviral activity of 2'- and 6'-fluoro carbocyclic pyrimidine nucleosides including carbocyclic 1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)-5-methyluracil and carbocyclic 1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)-5-iodouracil
Published in Journal of medicinal chemistry (01-01-1990)“…The racemic carbocyclic 2'-fluoroarabinosyl pyrimidine nucleosides 8, 9 (C-FIAU), 12, and 13 (C-FMAU) and the 2'-fluororibosyl pyrimidine nucleosides 17, 20,…”
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Identification and Characterization of a Herpes Simplex Virus Gene Product Required for Encapsidation of Virus DNA
Published in Journal of Virology (01-03-1983)“…Article Usage Stats Services JVI Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Penicillin derived C2-symmetric dimers as novel inhibitors of HIV-1 proteinase
Published in Journal of medicinal chemistry (01-08-1992)Get full text
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Structural basis for a new mechanism of inhibition of HIV-1 integrase identified by fragment screening and structure-based design
Published in Antiviral chemistry & chemotherapy (07-03-2011)“…HIV-1 integrase is a clinically validated therapeutic target for the treatment of HIV-1 infection, with one approved therapeutic currently on the market. This…”
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Fluorocarbocyclic nucleosides: synthesis and antiviral activity of 2'- and 6'-fluorocarbocyclic 2'-deoxyguanosines
Published in Journal of medicinal chemistry (01-03-1991)Get full text
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Genetic and biochemical studies with temperature-sensitive mutants of herpes simplex virus type 1
Published 01-01-1982“…The work presented in this thesis describes the isolation of a series of temperature-sensitive (1s) mutants of herpes simplex virus type 1 (HSV-1), Glasgow…”
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Dissertation