A novel orally active inhibitor of IL-1 generation: synthesis and structure-activity relationships of 3-(4-hydroxy-1-naphthalenyl)-2-propenoic acid derivatives

…, T Kaneko, K Tagami, S Hibi, Y Okamoto…

Index: Tanaka; Chiba; Okita; Kaneko; Tagami; Hibi; Okamoto; Shirota; Goto; Obaishi; Sakurai; Machida; Yamatsu Journal of Medicinal Chemistry, 1992 , vol. 35, # 25 p. 4665 - 4675

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Citation Number: 10

Abstract

A new series of 3-(4-hydroxy-l-naphthalenyl)-2-propenoic acids was prepared and the inhibitory activities of its members on IL-1 generation were evaluated both by in vitro systems using human monocytes and/or rat exudated macrophages stimulated with LPS, and by an in vivo system using the rat CMC-LPS air-pouch model. Many compounds in this series were found to be potent inhibitors of IL-1 generation both in vitro and in vivo. ...