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

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.

SUBMITTER: Knerr L

PROVIDER: S-EPMC6047051 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature

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

Knerr Laurent L Giordanetto Fabrizio F Nordberg Peter P Pettersen Daniel D Selmi Nidhal N Beisel Hans-Georg HG de la Motte Hannah H Olsson Thomas T Perkins Tim D J TDJ Herslöf Margareta M Månsson Åsa Å Dahlström Mikael M Starke Ingemar I Broddefalk Johan J Saarinen Gabrielle G Klingegård Fredrik F Hurt-Camejo Eva E Rosengren Birgitta B Brengdahl Johan J Jansen Frank F Rohman Mattias M Sandmark Jenny J Hallberg Kenth K Åkerud Tomas T Roth Robert G RG Ahlqvist Marie M

ACS medicinal chemistry letters 20180623 7

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. ...[more]

PMID: 30034585

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