European Journal of Medicinal Chemistry p. 187 - 198 (1996)
Update date:2022-08-04
Topics:
Tanaka
Okita
Akamatsu
Chiba
Obaishi
Nagakura
Sakurai
Yamatsu
A series of (E)-3-(7-hydroxy-6-methoxyindole-4-yl)-2-methylpropenoic acid derivatives was prepared and the inhibitory activities of its members on IL-1 generation were evaluated in an in vitro system using exudate cells from the rat carboxy-methyl cellulose (CMC) induced air-pouch model. All the compounds in this new series were found to be inhibitors of IL-1 generation. In particular, the methoxy-substituted 2-phenyl compounds 28d-f were the most potent inhibitors of IL-1 generation (eg, 28d: IC50 = 0.8 μ,M). The compounds in this series also inhibited IL-1α and IL-1β generations in an in vitro system using human monocytes stimulated with LPS (eg, 28b: IC50 = 1.4 μM (IL-1α) and 0.9 μM (IL-1β)).
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