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Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-06-23 , 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
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-06-23 , 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
Affiliation
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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.
中文翻译：
发现了一系列作为选择性分泌磷脂酶A2型X（sPLA2-X）抑制剂的吲哚2羧酰胺。
为了评估sPLA2-X作为动脉粥样硬化治疗靶标的潜力，需要具有改进的X型选择性的新型sPLA2抑制剂。为了实现鉴定此类化合物的目的，我们着手进行了先导研究，最终确定了一系列新颖的吲哚-2-羧酰胺作为选择性sPLA2-X抑制剂，具有进一步优化的潜力。
更新日期：2018-06-23
中文翻译：
发现了一系列作为选择性分泌磷脂酶A2型X（sPLA2-X）抑制剂的吲哚2羧酰胺。
为了评估sPLA2-X作为动脉粥样硬化治疗靶标的潜力，需要具有改进的X型选择性的新型sPLA2抑制剂。为了实现鉴定此类化合物的目的，我们着手进行了先导研究，最终确定了一系列新颖的吲哚-2-羧酰胺作为选择性sPLA2-X抑制剂，具有进一步优化的潜力。
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