Hydroxyindole derivatives as inhibitors of IL-1 generation. II. Synthesis and pharmacological activities of (E)-3-(7-hydroxy-6-methoxyindole-4-yl)-2-methylpropenoic …

…, H Obaishi, N Nagakura, H Sakurai, I Yamatsu

Index: Tanaka; Okita; Akamatsu; Chiba; Obaishi; Nagakura; Sakurai; Yamatsu European Journal of Medicinal Chemistry, 1996 , vol. 31, # 3 p. 187 - 198

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Abstract

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 carboxymethyl 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 ...