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

doi:10.1248/cpb.59.783

Notes

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

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Keywords: bistrifluoromethylpyridine, sulfonamide, secretory phospholipase A₂ inhibitor, structure–activity relationship

JOURNAL FREE ACCESS

2011 Volume 59 Issue 6 Pages 783-786

DOI https://doi.org/10.1248/cpb.59.783

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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 IC₅₀ value of 0.58 mM.

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