title: Design, synthesis and antifibrotic activities of carbohydrate-modified 1-(substituted aryl)-5-trifluoromethyl-2(1H) pyridones.
abstract: Pirfenidone, a pyridone compound, is an effective and novel antifibrotic agent. In this article, we describe the design, synthesis and activity evaluation of novel antifibrotic agents, 1-(substituted aryl)-5-trifluoromethyl-2(1H) pyridones modified with carbohydrate. Most of the title compounds exhibited comparable or better inhibitory activity than fluorofenidone. Notably, compound 19a demonstrated the highest cell-based inhibitory activity against NIH 3T3 (IC(50) = 0.17 mM).
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drug, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Qinghua
authors.initials: Q
authors.lastname: Lou
authors.forename: Xiangbao
authors.initials: X
authors.lastname: Meng
authors.forename: Zhiqi
authors.initials: Z
authors.lastname: Lao
authors.forename: Lingling
authors.initials: L
authors.lastname: Xuan
authors.forename: Jinye
authors.initials: J
authors.lastname: Bai
authors.forename: Qi
authors.initials: Q
authors.lastname: Hou
authors.forename: Gaoyun
authors.initials: G
authors.lastname: Hu
authors.forename: Renna
authors.initials: R
authors.lastname: Luo
authors.forename: Lijian
authors.initials: L
authors.lastname: Tao
authors.forename: Zhongjun
authors.initials: Z
authors.lastname: Li
mesh_terms: D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects*; D015195:Drug Design; D005355:Fibrosis / Q000188:drug therapy; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D051379:Mice; D009005:Monosaccharides / Q000737:chemistry*; D041681:NIH 3T3 Cells; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D012995:Solubility
chemical_list: C511655:5-methyl-1-(3-fluorophenyl)-2-(1H)-pyridone; D009005:Monosaccharides; D011728:Pyridones; C093844:pirfenidone