Synthesis of N-(Trifluoromethyl-2-pyridinyl)arenesulfonamides as an Inhibitor of Secretory Phospholipase A2

Hitoshi Nakayama, Yuka Morita, Hirohiko Kimura, Keiichi Ishihara, Satoshi Akiba, Jun'ichi Uenishi
2011 Chemical and pharmaceutical bulletin  
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 A 2 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.
doi:10.1248/cpb.59.783 pmid:21628920 fatcat:wyncl7qg7bg63ks4bbk67o45dy