{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Gu C"],"funding":["Natural Science Foundation of Shandong Province"],"pagination":["14492-14501"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9102048"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["12(23)"],"pubmed_abstract":["Two series of new pirfenidone derivatives, in which phenyl groups or benzyl groups are attached to the nitrogen atom of the pyridin-2(1<i>H</i>)-one moiety were synthesized and evaluated as anti-fibrosis agents. Among them, compound 5d, with a (<i>S</i>)-2-(dimethylamino) propanamido group in the R<sub>2</sub> position (series 1) exhibited 10 times the anti-fibrosis activity (IC<sub>50</sub>: 0.245 mM) of pirfenidone (IC<sub>50</sub>: 2.75 mM). Compound 9d (series 2) gave an IC<sub>50</sub> of 0.035 mM against the human fibroblast cell line HFL1. The mechanism of the optimal compound inhibiting fibrosis was also studied."],"journal":["RSC advances"],"pubmed_title":["Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents."],"pmcid":["PMC9102048"],"funding_grant_id":["ZR2021QB172"],"pubmed_authors":["Li W","An B","Li X","Gu C","Yang L","Hu W","Yao H","Ju Q"],"additional_accession":[]},"is_claimable":false,"name":"Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents.","description":"Two series of new pirfenidone derivatives, in which phenyl groups or benzyl groups are attached to the nitrogen atom of the pyridin-2(1<i>H</i>)-one moiety were synthesized and evaluated as anti-fibrosis agents. Among them, compound 5d, with a (<i>S</i>)-2-(dimethylamino) propanamido group in the R<sub>2</sub> position (series 1) exhibited 10 times the anti-fibrosis activity (IC<sub>50</sub>: 0.245 mM) of pirfenidone (IC<sub>50</sub>: 2.75 mM). Compound 9d (series 2) gave an IC<sub>50</sub> of 0.035 mM against the human fibroblast cell line HFL1. The mechanism of the optimal compound inhibiting fibrosis was also studied.","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 May","modification":"2026-05-10T01:39:54.513Z","creation":"2025-02-19T01:12:36.896Z"},"accession":"S-EPMC9102048","cross_references":{"pubmed":["35702193"],"doi":["10.1039/d2ra00990k"]}}