Preparation and Antirheumatic Activity of Optically Active 2-Acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic Acid (KE-298)
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概要
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2-Acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanonic acid (KE-298) is an antirheumatic agent. To elucidate the effects of optically active KE-298,we resolved the racemic acid and obtained the two optical isomers. (+)-KE-298 was converted to the 4-bromobenzyl ester derivative and the absolute structure was confirmed as (S) by X-ray crystallographic analysis.The pharmacological activities of the optical isomers and racemic KE-298 were compared by using the characteristic tests for KE-298. Though (+)-KE-298 showed a stronger suppressive effect on rat adjuvant arthritis than (-)-KE-298,no difference between the two isomers was detected in in vitro tests (enhancing effect on lymphocyte transformation, IL-1 antagonistic effect).
- 1996-03-15
著者
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Yasuda Yoshiko
Research Center Taisho Pharmaceutical Co. Ltd.
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Matsumoto Keita
Research Center Taisho Pharmaceutical Co. Ltd.
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KAMEO Kazuya
Research Center, Taisho Pharmaceutical Co., Ltd.,
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TAKESHITA Kimiyo
Research Center, Taisho Pharmaceutical Co., Ltd.,
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TOMISAWA Kazuyuki
Research Center, Taisho Pharmaceutical Co., Ltd.,
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Tomisawa Kazuyuki
Research Center Taisho Pharmaceutical Co. Ltd.
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Kameo K
Research Center Taisho Pharmaceutical Co. Ltd.
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Takeshita K
Sci. Univ. Tokyo Tokyo Jpn
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- Preparation and Antirheumatic Activity of Optically Active 2-Acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic Acid (KE-298)
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