Preparation and antirheumatic activity of optically active 2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (KE-298).
Chem Pharm Bull (Tokyo)
; 44(3): 602-4, 1996 Mar.
Article
em En
| MEDLINE
| ID: mdl-8882457
ABSTRACT
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).
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Fenilpropionatos
/
Antirreumáticos
Limite:
Animals
Idioma:
En
Revista:
Chem Pharm Bull (Tokyo)
Ano de publicação:
1996
Tipo de documento:
Article
País de afiliação:
Japão