2. Academic Validation
  3. Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors

Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors

  • ACS Med Chem Lett. 2018 Jun 23;9(7):594-599. doi: 10.1021/acsmedchemlett.7b00505.
Laurent Knerr 1,  Fabrizio Giordanetto 1,  Peter Nordberg 1,  Daniel Pettersen 1,  Nidhal Selmi 1,  Hans-Georg Beisel 1,  Hannah de la Motte 1,  Thomas Olsson 1,  Tim D J Perkins 1,  Margareta Herslöf 1,  Åsa Månsson 1,  Mikael Dahlström 1,  Ingemar Starke 1,  Johan Broddefalk 1,  Gabrielle Saarinen 1,  Fredrik Klingegård 1,  Eva Hurt-Camejo 1,  Birgitta Rosengren 1,  Johan Brengdahl 2,  Frank Jansen 2,  Mattias Rohman 2,  Jenny Sandmark 2,  Kenth Hallberg 2,  Tomas Åkerud 2,  Robert G Roth 2,  Marie Ahlqvist 1
Affiliations

Affiliations

  • 1 Medicinal Chemistry, Translational Sciences, Bioscience and Drug Metabolism and Pharmacokinetics, Cardiovascular and Metabolic Diseases, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
  • 2 Reagents and Assay Development, Mechanistic Biology and Profiling, and Structure and Biophysics, Discovery Sciences, IMED Biotech Unit, AstraZeneca, Gothenburg SE-431 89, Sweden.
PMID: 30034585 DOI: 10.1021/acsmedchemlett.7b00505
Abstract

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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