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Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors.

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Title: Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors.
Authors: Thomas MG; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., McGonagle K; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Rowland P; GlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY., Robinson DA; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Dodd PG; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Camino-Díaz I; GlaxoSmithKline, Discovery DMPK, IVIVT, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain., Campbell L; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Cantizani J; GlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain., Castañeda P; GlaxoSmithKline, Discovery DMPK, IVIVT, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain., Conn D; GlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY., Craggs PD; GlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY., Edwards D; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Ferguson L; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Fosberry A; GlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY., Frame L; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Goswami P; GlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY., Hu X; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Korczynska J; GlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY., MacLean L; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Martin J; GlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain., Mutter N; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Osuna-Cabello M; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Paterson C; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Peña I; GlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain., Pinto EG; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Pont C; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Riley J; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Shishikura Y; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Simeons FRC; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Stojanovski L; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Thomas J; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Wrobel K; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Young RJ; Blue Burgundy Ltd, Ampthill, Bedfordshire, U.K., MK45 2AD., Zmuda F; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Zuccotto F; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Read KD; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Gilbert IH; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH., Marco M; GlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain., Miles TJ; GlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain., Manzano P; GlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain., De Rycker M; Drug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Source: Journal of medicinal chemistry [J Med Chem] 2023 Aug 10; Vol. 66 (15), pp. 10413-10431. Date of Electronic Publication: 2023 Jul 28.
Publication Type: Journal Article; Research Support, Non-U.S. Gov't
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
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