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(1H)-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 (s...

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Detalles Bibliográficos
Autores principales: Gu, Chenxi, Li, Wei, Ju, Qing, Yao, Han, Yang, Lisheng, An, Baijiao, Hu, Wenhao, Li, Xingshu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2022
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9102048/
https://www.ncbi.nlm.nih.gov/pubmed/35702193
http://dx.doi.org/10.1039/d2ra00990k
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author Gu, Chenxi
Li, Wei
Ju, Qing
Yao, Han
Yang, Lisheng
An, Baijiao
Hu, Wenhao
Li, Xingshu
author_facet Gu, Chenxi
Li, Wei
Ju, Qing
Yao, Han
Yang, Lisheng
An, Baijiao
Hu, Wenhao
Li, Xingshu
author_sort Gu, Chenxi
collection PubMed
description 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 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.
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spelling pubmed-91020482022-06-13 Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents Gu, Chenxi Li, Wei Ju, Qing Yao, Han Yang, Lisheng An, Baijiao Hu, Wenhao Li, Xingshu RSC Adv Chemistry 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 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. The Royal Society of Chemistry 2022-05-13 /pmc/articles/PMC9102048/ /pubmed/35702193 http://dx.doi.org/10.1039/d2ra00990k Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/
spellingShingle Chemistry
Gu, Chenxi
Li, Wei
Ju, Qing
Yao, Han
Yang, Lisheng
An, Baijiao
Hu, Wenhao
Li, Xingshu
Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents
title Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents
title_full Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents
title_fullStr Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents
title_full_unstemmed Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents
title_short Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents
title_sort synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9102048/
https://www.ncbi.nlm.nih.gov/pubmed/35702193
http://dx.doi.org/10.1039/d2ra00990k
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