24680-31-7Relevant academic research and scientific papers
NOVEL THIOPHENE COMPOUNDS, PROCESS FOR SYNTHESIS AND USE THEREOF
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Paragraph 0059; 0056, (2019/03/17)
The present invention relates to novel thiophene compounds of general Formula I, and their stereoisomers (diastereoisomers, enantiomers), pure or mixed, racemic mixtures, geometrical isomers, tautomers, pharmaceutically acceptable salts, hydrates, solvate
Synthesis and structure-activity relationships of 5-phenylthiophenecarboxylic acid derivatives as antirheumatic agents
Noguchi, Toshiya,Hasegawa, Masahiro,Tomisawa, Kazuyuki,Mitsukuchi, Morihiro
, p. 4729 - 4742 (2007/10/03)
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 compared with those of 1. The structure-activity relationships indicated that [5-(4-bromophenyl)-thiophen-3-yl]acetic acid (5d), methyl [5-(4-chlorophenyl)-thiophen-3-yl]acetate (5h), and methyl [5-(4-bromophenyl)-thiophen-3-yl]acetate (5i) suppressed AIA more potently than 1 and all of the other synthesized compounds.
