1. Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors
- Author
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Tomas Akerud, Hannah de la Motte, Eva Hurt-Camejo, Tim D. J. Perkins, Åsa Månsson, Frank Jansen, Hans-Georg Beisel, Mikael Dahlström, Gabrielle Saarinen, Fabrizio Giordanetto, Robert G. Roth, Marie Ahlqvist, Fredrik Klingegård, Birgitta Rosengren, Laurent Knerr, Kenth Hallberg, Ingemar Starke, Jenny Sandmark, Daniel Pettersen, Nidhal Selmi, Margareta Herslöf, Johan Brengdahl, Tommy Olsson, Mattias Rohman, Peter Nordberg, and Johan Broddefalk
- Subjects
0301 basic medicine ,Indole test ,biology ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,01 natural sciences ,Biochemistry ,Combinatorial chemistry ,0104 chemical sciences ,03 medical and health sciences ,030104 developmental biology ,Phospholipase A2 ,Drug Discovery ,biology.protein ,Selectivity - Abstract
[Image: see text] In order to assess the potential of sPLA(2)-X as a therapeutic target for atherosclerosis, novel sPLA(2) 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.
- Published
- 2018
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