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Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors.
Knerr, Laurent; Giordanetto, Fabrizio; Nordberg, Peter; Pettersen, Daniel; Selmi, Nidhal; Beisel, Hans-Georg; de la Motte, Hannah; Olsson, Thomas; Perkins, Tim D J; Herslöf, Margareta; Månsson, Åsa; Dahlström, Mikael; Starke, Ingemar; Broddefalk, Johan; Saarinen, Gabrielle; Klingegård, Fredrik; Hurt-Camejo, Eva; Rosengren, Birgitta; Brengdahl, Johan; Jansen, Frank; Rohman, Mattias; Sandmark, Jenny; Hallberg, Kenth; Åkerud, Tomas; Roth, Robert G; Ahlqvist, Marie.
Afiliação
  • Knerr L; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Giordanetto F; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Nordberg P; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Pettersen D; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Selmi N; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Beisel HG; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • de la Motte H; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Olsson T; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Perkins TDJ; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Herslöf M; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Månsson Å; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Dahlström M; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Starke I; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Broddefalk J; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Saarinen G; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Klingegård F; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Hurt-Camejo E; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Rosengren B; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Brengdahl J; Reagents and Assay Development, Mechanistic Biology and Profiling, and Structure and Biophysics, Discovery Sciences, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Jansen F; Reagents and Assay Development, Mechanistic Biology and Profiling, and Structure and Biophysics, Discovery Sciences, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Rohman M; Reagents and Assay Development, Mechanistic Biology and Profiling, and Structure and Biophysics, Discovery Sciences, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Sandmark J; Reagents and Assay Development, Mechanistic Biology and Profiling, and Structure and Biophysics, Discovery Sciences, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Hallberg K; Reagents and Assay Development, Mechanistic Biology and Profiling, and Structure and Biophysics, Discovery Sciences, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Åkerud T; Reagents and Assay Development, Mechanistic Biology and Profiling, and Structure and Biophysics, Discovery Sciences, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Roth RG; Reagents and Assay Development, Mechanistic Biology and Profiling, and Structure and Biophysics, Discovery Sciences, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • Ahlqvist M; Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
ACS Med Chem Lett ; 9(7): 594-599, 2018 Jul 12.
Article em En | MEDLINE | ID: mdl-30034585
In order to assess the potential of sPLA2-X as a therapeutic target for atherosclerosis, novel sPLA2 inhibitors with improved type X selectivity are required. To achieve the objective of identifying such compounds, we embarked on a lead generation effort that resulted in the identification of a novel series of indole-2-carboxamides as selective sPLA2-X inhibitors with excellent potential for further optimization.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2018 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2018 Tipo de documento: Article