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ID: ALA2057179

Journal: Bioorg Med Chem Lett

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

Authors: Hansen FK, Khankischpur M, Tolaymat I, Mesaros R, Dannhardt G, Geffken D.

Abstract: 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 IC(50) values for inhibition of 5-LOX and COX-1, respectively.

CiteXplore: 22749420

DOI: 10.1016/j.bmcl.2012.06.012