Discovery of AZD2716: A Novel Secreted Phospholipase A(2) (sPLA(2)) Inhibitor for the Treatment of Coronary Artery Disease

[Image: see text] Expedited structure-based optimization of the initial fragment hit 1 led to the design of (R)-7 (AZD2716) a novel, potent secreted phospholipase A(2) (sPLA(2)) inhibitor with excellent preclinical pharmacokinetic properties across species, clear in vivo efficacy, and minimized safe...

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Detalles Bibliográficos
Autores principales: Giordanetto, Fabrizio, Pettersen, Daniel, Starke, Ingemar, Nordberg, Peter, Dahlström, Mikael, Knerr, Laurent, Selmi, Nidhal, Rosengren, Birgitta, Larsson, Lars-Olof, Sandmark, Jenny, Castaldo, Marie, Dekker, Niek, Karlsson, Ulla, Hurt-Camejo, Eva
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5066155/
https://www.ncbi.nlm.nih.gov/pubmed/27774123
http://dx.doi.org/10.1021/acsmedchemlett.6b00188
Descripción
Sumario:[Image: see text] Expedited structure-based optimization of the initial fragment hit 1 led to the design of (R)-7 (AZD2716) a novel, potent secreted phospholipase A(2) (sPLA(2)) inhibitor with excellent preclinical pharmacokinetic properties across species, clear in vivo efficacy, and minimized safety risk. Based on accumulated profiling data, (R)-7 was selected as a clinical candidate for the treatment of coronary artery disease.

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