Synthesis of N-[2-(2, 4-Difluorophenoxy) trifluoromethyl-3-pyridyl] sulfonamides and Their Inhibitory Activities against Secretory Phospholipase A2

H Nakayama, K Ishihara, S Akiba…

Index: Nakayama, Hitoshi; Ishihara, Keiichi; Akiba, Satoshi; Uenishi, Jun'ichi Chemical and Pharmaceutical Bulletin, 2011 , vol. 59, # 8 p. 1069 - 1072

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Citation Number: 6

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 A 2 (sPLA 2) were examined and N-[2-(2, 4-difluorophenoxy)-5-trifluoromethyl-3-pyridyl]-2-naphthalenesulfonamide (5c) was found to be the most potent against sPLA 2 with an IC 50 value of 90 μM.