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.
Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A(2) Type X (sPLA(2)-X) Inhibitors.
发现一系列吲哚-2 甲酰胺类化合物作为选择性分泌型磷脂酶 A(2) X 型 (sPLA(2)-X) 抑制剂
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作者:Knerr Laurent, Giordanetto Fabrizio, Nordberg Peter, Pettersen Daniel, Selmi Nidhal, Beisel Hans-Georg, de la Motte Hannah, Olsson Thomas, Perkins Tim D J, Herslöf Margareta, MÃ¥nsson à sa, Dahlström Mikael, Starke Ingemar, Broddefalk Johan, Saarinen Gabrielle, KlingegÃ¥rd Fredrik, Hurt-Camejo Eva, Rosengren Birgitta, Brengdahl Johan, Jansen Frank, Rohman Mattias, Sandmark Jenny, Hallberg Kenth, à kerud Tomas, Roth Robert G, Ahlqvist Marie
| 期刊: | ACS Medicinal Chemistry Letters | 影响因子: | 4.000 |
| 时间: | 2018 | 起止号: | 2018 Jun 23; 9(7):594-599 |
| doi: | 10.1021/acsmedchemlett.7b00505 | 研究方向: | 信号转导 |
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