title: Synthesis of N-[2-(2,4-Difluorophenoxy)trifluoromethyl-3-pyridyl]sulfonamides and their inhibitory activities against secretory phospholipase A₂.
abstract: N-[2-(2,4-Difluorophenoxy)trifluoromethyl-3-pyridyl]sulfonamide derivatives 3-6 were prepared by the reaction of 3-pyridylamines and sulfonyl chlorides. Inhibitory activities of these compounds toward secretory phospholipase A₂ (sPLA₂) were examined and N-[2-(2,4-difluorophenoxy)-5-trifluoromethyl-3-pyridyl]-2-naphthalenesulfonamide (5c) was found to be the most potent against sPLA₂ with an IC₅₀ value of 90 µM.
authors.affiliation: Department of Pharmaceutical Chemistry, Kyoto Pharmaceutical University, Japan. hi-nakayama@iskweb.co.jp
authors.forename: Hitoshi
authors.initials: H
authors.lastname: Nakayama
authors.forename: Keiichi
authors.initials: K
authors.lastname: Ishihara
authors.forename: Satoshi
authors.initials: S
authors.lastname: Akiba
authors.forename: Jun'ichi
authors.initials: J
authors.lastname: Uenishi
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D054497:Phospholipases A2, Secretory / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D013449:Sulfonamides; C095186:trifluoromethylsulfonamide; C051353:naphthalenesulfonamide; D054497:Phospholipases A2, Secretory