Issue 23, 2022
From the journal:

RSC Advances

Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents†

Chenxi Gu,a   Wei Li,a   Qing Ju,b   Han Yao,a   Lisheng Yang,a   Baijiao An,*b   Wenhao Hu*a  and  Xingshu Li ORCID logo a  

* Corresponding authors

a School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, PR China
E-mail: huwh9@mail.sysu.edu.cn

b Medicine and Pharmacy Research Center, Binzhou Medical University, Yantai, Shandong Province, PR China

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.

Graphical abstract: Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents

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Article information

DOI
https://doi.org/10.1039/D2RA00990K
Article type
Paper
Submitted
15 Feb 2022
Accepted
16 Apr 2022
First published
13 May 2022
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2022,12, 14492-14501

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Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents

C. Gu, W. Li, Q. Ju, H. Yao, L. Yang, B. An, W. Hu and X. Li, RSC Adv., 2022, 12, 14492 DOI: 10.1039/D2RA00990K

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