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

Autor: 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.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2023 Aug 10; Vol. 66 (15), pp. 10413-10431. Date of Electronic Publication: 2023 Jul 28.

Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.

Autor: Thomas M; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Brand S; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., De Rycker M; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Zuccotto F; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Lukac I; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Dodd PG; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Ko EJ; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Manthri S; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., McGonagle K; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Osuna-Cabello M; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Riley J; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Pont C; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Simeons F; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Stojanovski L; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Thomas J; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Thompson S; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Viayna E; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Fiandor JM; Global Health R&D, GlaxoSmithKline, Tres Cantos 28760, Spain., Martin J; Global Health R&D, GlaxoSmithKline, Tres Cantos 28760, Spain., Wyatt PG; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Miles TJ; Global Health R&D, GlaxoSmithKline, Tres Cantos 28760, Spain., Read KD; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K., Marco M; Global Health R&D, GlaxoSmithKline, Tres Cantos 28760, Spain., Gilbert IH; Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2021 May 13; Vol. 64 (9), pp. 5905-5930. Date of Electronic Publication: 2021 Apr 27.

TAK1 inhibition in the DFG-out conformation.

Autor: Kilty I; Pfizer World Wide Research and Development, Ramsgate Road, Sandwich, CT13 9NJ, UK; BioTherapeutics Research and Development, Pfizer, Cambridge, MA, 02140, USA., Green MP, Bell AS, Brown DG, Dodd PG, Hewson C, Hughes SJ, Phillips C, Ryckmans T, Smith RT, van Hoorn WP, Cohen P, Jones LH

Publikováno v: Chemical biology & drug design [Chem Biol Drug Des] 2013 Nov; Vol. 82 (5), pp. 500-5.

In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.

Autor: Mantell SJ; Drug Discovery Group, Medical Research Council Technology, Mill Hill, London, United Kingdom. simon.mantell@pfizer.com, Gibson KR, Osborne SA, Maw GN, Rees H, Dodd PG, Greener B, Harbottle GW, Million WA, Poinsard C, England S, Carnell P, Betts AM, Monhemius R, Prime RL

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Apr 15; Vol. 19 (8), pp. 2190-4. Date of Electronic Publication: 2009 Mar 03.

Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.

Autor: Owen DR; Pfizer Global Research and Development, Ramsgate Road, Sandwich, CT13 9NJ, UK. dafydd.owen@pfizer.com, Dodd PG, Gayton S, Greener BS, Harbottle GW, Mantell SJ, Maw GN, Osborne SA, Rees H, Ringer TJ, Rodriguez-Lens M, Smith GF

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jan 15; Vol. 17 (2), pp. 486-90. Date of Electronic Publication: 2006 Oct 11.