Unknown

Dataset Information

0

Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents.

ABSTRACT: 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 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.

SUBMITTER: Gu C 

PROVIDER: S-EPMC9102048 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Synthesis and evaluation of new pirfenidone derivatives as anti-fibrosis agents.

Gu Chenxi C   Li Wei W   Ju Qing Q   Yao Han H   Yang Lisheng L   An Baijiao B   Hu Wenhao W   Li Xingshu X  

RSC advances 20220513 23

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  ...[more]

Similar Datasets

Unknown Synthesis and structure-activity relationships of pirfenidone derivatives as anti-fibrosis agents <i>in vitro</i>.
| S-EPMC9132227 | biostudies-literature
Unknown Synthesis and biological evaluation of new ligustrazine derivatives as anti-tumor agents.
| S-EPMC6268357 | biostudies-literature
Unknown Novel pirfenidone derivatives: synthesis and biological evaluation.
| S-EPMC10285743 | biostudies-literature
Unknown Design, synthesis and biological evaluation of new carbazole derivatives as anti-cancer and anti-migratory agents.
| S-EPMC5822041 | biostudies-literature
Unknown N-thioalkylcarbazoles derivatives as new anti-proliferative agents: synthesis, characterisation and molecular mechanism evaluation.
| S-EPMC6010102 | biostudies-literature
Unknown Indolylmaleimide derivatives as a new class of anti-leishmanial agents: synthesis and biological evaluation.
| S-EPMC12004262 | biostudies-literature
Unknown Synthesis and Evaluation of New Coumarin Derivatives as Antioxidant, Antimicrobial, and Anti-Inflammatory Agents.
| S-EPMC7397269 | biostudies-literature
Unknown Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents.
| S-EPMC8121267 | biostudies-literature
Unknown Synthesis and biological evaluation of new 3-amino-2-azetidinone derivatives as anti-colorectal cancer agents.
| S-EPMC6071799 | biostudies-literature
Unknown Design, Synthesis, and Anti-Hepatic Fibrosis Evaluation of Cordycepin Derivatives.
| S-EPMC12844307 | biostudies-literature