Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo [b] thiophene-2-carboxylic acid derivatives

…, I Tolaymat, R Mesaros, G Dannhardt, D Geffken

文献索引：Hansen, Finn K.; Khankischpur, Mehdi; Tolaymat, Ibrahim; Mesaros, Renata; Dannhardt, Gerd; Geffken, Detlef Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 15 p. 5031 - 5034

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被引用次数: 3

摘要

A series of 3-hydroxybenzo [b] thiophene-2-carboxylic acid derivatives has been prepared and subsequently evaluated with regards to the inhibition of 5-LOX/COX. Structure optimization furnished derivatives with promising in vitro activity as dual 5-LOX/COX inhibitors with submicromolar IC50 values for inhibition of 5-LOX and COX-1, respectively.