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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
Author(s) -
Katila Pramila,
Shrestha Aastha,
Shrestha Aarajana,
Shrestha Ritina,
Park PilHoon,
Lee EungSeok
Publication year - 2018
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.11618
Subject(s) - moiety , chemistry , stereochemistry , inhibitory postsynaptic potential , biology , neuroscience
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 IC 50 value of 3.29 μM.