Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents. Issue 23 (13th May 2022)

• Record Type: Journal Article
• Authors: Gu, Chenxi; Li, Wei; Ju, Qing; Yao, Han; Yang, Lisheng; An, Baijiao; Hu, Wenhao; Li, Xingshu
• Is Part Of: RSC advances. Volume 12:Issue 23(2022)
• Page Start: 14492
• Page End: 14501
• Publication Date: 2022-05-13
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/d2ra00990k
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : Two series of new pirfenidone derivatives were synthesized and evaluated as anti-fibrosis agents. Among them, compound 9d give 35 μM of the IC50 against the human fibroblast cell line HFL1. 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 H )-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.