Design and Synthesis of Fluorinated and/or Hydroxylated 2‐Arylidene‐1‐indanone Derivatives as an Inhibitor of LPS‐stimulated ROS Production in RAW 264.7 Macrophages with Structure–Activity Relationship Study

Bulletin of the Korean Chemical Society

Pramila Katila¹ 

[1] College of Pharmacy Yeungnam University Gyeongsan 712749 Republic of Korea

关键词: 2‐;    arylidene‐;    1‐;    indanone;    Reduction of ROS in LPS‐;    stimulated RAW 264.7 macrophages;   

DOI  :  10.1002/bkcs.11618

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

A new series of thirty‐two fluorinated and/or hydroxylated 2‐arylidene‐1‐indanone derivatives were systematically designed, synthesized, and evaluated for their inhibitory activity against LPS‐stimulated ROS production in RAW 264.7 macrophages. 5/6‐Fluoro‐1‐indanone or 4‐, 5‐, 6‐, or 7‐hydroxyindanone moiety along with ortho‐, meta‐, or para‐hydroxyphenyl, furanyl or thiophenyl moiety was prepared and evaluated. Among the synthesized compounds, compound 11 possessing 6‐hydroxy‐1‐indanone moiety along with 5‐chlorothiophenyl moiety was found to have the most potent inhibitory effect on the production of ROS in LPS‐stimulated RAW 264.7 macrophages with an IC50 value of 3.29 μM.

【 授权许可】

Unknown