title: Synthesis of N-(trifluoromethyl-2-pyridinyl)arenesulfonamides as an inhibitor of secretory phospholipase A₂.
abstract: A series of N-(trifluoromethyl-2-pyridinyl)alkane- and arenesulfonamides 2-5 have been synthesized by the substitution reaction of 2-chloro(trifluoromethyl)pyridines 6 with alkane- and arenesulfonamides 7. Their inhibitory activities against secretory phospholipase A₂ of porcine pancreas were examined and the analog N-[4,5-bis(trifluoromethyl)-2-pyridinyl]-4-trifluoromethylbenzenesulfonamide 4i was shown to have the highest inhibitory activity, with an IC(50) value of 0.58 mM.
authors.affiliation: Department of Pharmaceutical Chemistry, Kyoto Pharmaceutical University, Misasagi, Yamashina, Kyoto, Japan. hi-nakayama@iskweb.co.jp
authors.forename: Hitoshi
authors.initials: H
authors.lastname: Nakayama
authors.forename: Yuka
authors.initials: Y
authors.lastname: Morita
authors.forename: Hirohiko
authors.initials: H
authors.lastname: Kimura
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: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010179:Pancreas / Q000201:enzymology; D054497:Phospholipases A2, Secretory / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011725:Pyridines / Q000737:chemistry*; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013552:Swine
chemical_list: D004791:Enzyme Inhibitors; D011725:Pyridines; D013449:Sulfonamides; C407065:trifluoromethylpyridine; D054497:Phospholipases A2, Secretory