Synthesis and structure–activity relationships of 5-phenylthiophenecarboxylic acid derivatives as antirheumatic agents

…, M Hasegawa, K Tomisawa, M Mitsukuchi

Index: Noguchi, Toshiya; Hasegawa, Masahiro; Tomisawa, Kazuyuki; Mitsukuchi, Morihiro Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 22 p. 4729 - 4742

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Citation Number: 15

Abstract

5-(Phenylthiophene)-3-carboxylic acid (2a), a metabolite of esonarimod (1), which was developed as a new antirheumatic drug, was considered as a lead compound for new antirheumatic drugs. A new series of 2a derivatives were synthesized and their characteristic pharmacological effects, that is their antagonistic effect toward interleukin (IL)-1 in mice and the suppressive effect against adjuvant-induced arthritis (AIA) in rats, were evaluated and ...