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

Two series of new pirfenidone derivatives, in which phenyl groups or benzyl groups are attached to the nitrogen atom of the pyridin-2(1 H )-one moiety were synthesized and evaluated as anti-fibrosis agents. Among them, compound 5d , with a ( S )-2-(dimethylamino) propanamido group in the R 2 positio...

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Published inRSC advances Vol. 12; no. 23; pp. 14492 - 1451
Main Authors Gu, Chenxi, Li, Wei, Ju, Qing, Yao, Han, Yang, Lisheng, An, Baijiao, Hu, Wenhao, Li, Xingshu
Format Journal Article
LanguageEnglish
Published England Royal Society of Chemistry 12.05.2022
The Royal Society of Chemistry
Subjects
Chemistry
Fibrosis
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Summary:Two series of new pirfenidone derivatives, in which phenyl groups or benzyl groups are attached to the nitrogen atom of the pyridin-2(1 H )-one moiety were synthesized and evaluated as anti-fibrosis agents. Among them, compound 5d , with a ( S )-2-(dimethylamino) propanamido group in the R 2 position (series 1) exhibited 10 times the anti-fibrosis activity (IC 50 : 0.245 mM) of pirfenidone (IC 50 : 2.75 mM). Compound 9d (series 2) gave an IC 50 of 0.035 mM against the human fibroblast cell line HFL1. The mechanism of the optimal compound inhibiting fibrosis was also studied. Two series of new pirfenidone derivatives were synthesized and evaluated as anti-fibrosis agents. Among them, compound 9d give 35 μM of the IC 50 against the human fibroblast cell line HFL1.
Bibliography:Electronic supplementary information (ESI) available. See
https://doi.org/10.1039/d2ra00990k
ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:2046-2069
2046-2069
DOI:10.1039/d2ra00990k