Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives
2012
Hansen, Finn K. | Khankischpur, Mehdi | Tolaymat, Ibrahim | Mesaros, Renata | Dannhardt, G. (Gerd) | Geffken, Detlef
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.
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