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

Hitoshi Nakayama; Keiichi Ishihara; Satoshi Akiba; Jun'ichi Uenishi

doi:10.1248/cpb.59.1069

Notes

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

Hitoshi Nakayama, Keiichi Ishihara, Satoshi Akiba, Jun'ichi Uenishi

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Keywords: trifluoromethylpyridine, sulfonamide, secretory phospholipase A₂ inhibitor, 2,4-difluorophenoxy, naphthalenesulfonamide

JOURNAL FREE ACCESS

2011 Volume 59 Issue 8 Pages 1069-1072

DOI https://doi.org/10.1248/cpb.59.1069

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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.

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