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Synthesis and biological evaluation of the pirfenidone derivatives as antifibrotic agents.

Abstract：

:A total of 24 pirfenidone derivatives were designed, synthesized and evaluated for their inhibitory activity against the human lung fibroblast cell line MRC-5. These compounds showed the remarkable proliferation inhibition against MRC-5 compared to pirfenidone as the positive control. The possible mechanism of this kind of derivatives as antifibrotic agents was explored. The molecular docking and p38 binding affinity assays demonstrated that the antifibrotic potential of the pirfenidone derivatives was possibly through the inhibition of p38 MAPK signaling pathway. The data from this study suggested that p38 might be a potential therapeutic target for the new generation antifibrotics. All the pirfenidone derivatives are reported here for the first time.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ma Z,Pan Y,Huang W,Yang Y,Wang Z,Li Q,Zhao Y,Zhang X,Shen Z

doi

10.1016/j.bmcl.2013.11.038

subject

Has Abstract

pub_date

2014-01-01 00:00:00

pages

220-3

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)01317-6

journal_volume

24

pub_type

杂志文章

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