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Updated: Sep 8, 2025

Unilateral Lung Volume Analysis Using Micro-CT for Enhanced Assessment of Pulmonary Fibrosis in Preclinical Models
Published on: June 20, 2025
Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents
1School of Pharmaceutical Sciences, Sun Yat-Sen University Guangzhou 510006 PR China huwh9@mail.sysu.edu.cn.
Abstract:
Two series of new pirfenidone derivatives, in which phenyl groups or benzyl groups are attached to the nitrogen atom of the pyridin-2(1H)-one moiety were synthesized and evaluated as anti-fibrosis agents. Among them, compound 5d, with a (S)-2-(dimethylamino) propanamido group in the R2 position (series 1) exhibited 10 times the anti-fibrosis activity (IC50: 0.245 mM) of pirfenidone (IC50: 2.75 mM). Compound 9d (series 2) gave an IC50 of 0.035 mM against the human fibroblast cell line HFL1. The mechanism of the optimal compound inhibiting fibrosis was also studied.
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