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...

Descripción completa

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
Descripción
Sumario: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.

Ejemplares similares