Synthesis and structure–activity relationships of pirfenidone derivatives as anti-fibrosis agents <i>in vitro</i>
Xiufang Shi, Zhenqiang Yu, Chaoran Zhu, Linlin Jiang, Nanqi Geng, Xingting Fan, Zhanghui Guan, Xiang Lü
Abstract
Total 18 PFD derivatives with the amide group replacing 5-methyl were synthesized and evaluated. YZQ17 possessed considerable antifibrosis activity in vitro via TGF-β/Smad2/3 pathway and was regarded as a lead compound for further optimization.
Topics & Concepts
PirfenidoneIn vitroFibrosisChemistryPharmacologyMedicineCombinatorial chemistryBiochemistryInternal medicineIdiopathic pulmonary fibrosisLungInterstitial Lung Diseases and Idiopathic Pulmonary FibrosisQuinazolinone synthesis and applicationsEosinophilic Disorders and Syndromes