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

Knerr L, Giordanetto F, Nordberg P, Pettersen D, Selmi N, Beisel HG, de la Motte H, Olsson T, Perkins TDJ, Herslöf M, Månsson Å, Dahlström M, Starke I, Broddefalk J, Saarinen G, Klingegård F, Hurt-Camejo E, Rosengren B, Brengdahl J, Jansen F, Rohman M, Sandmark J, Hallberg K, Åkerud T, Roth RG, Ahlqvist M

ACS Med. Chem. Lett. 9 (7) 594-599 [2018-07-12; online 2018-06-23]

In order to assess the potential of sPLA 2-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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PubMed 30034585

DOI 10.1021/acsmedchemlett.7b00505

Crossref 10.1021/acsmedchemlett.7b00505

pmc PMC6047051