Two series of new pirfenidone derivatives, in which phenyl groups or benzyl groups are attached to the nitrogen atom of the pyridin-2(1)-one moiety were synthesized and evaluated as anti-fibrosis agents. Among them, compound 5d, with a ()-2-(dimethylamino) propanamido group in the R position (series 1) exhibited 10 times the anti-fibrosis activity (IC: 0.245 mM) of pirfenidone (IC: 2.75 mM). Compound 9d (series 2) gave an IC 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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| http://dx.doi.org/10.1039/d2ra00990k | DOI Listing |
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