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Bioorg Med Chem Lett. 2012 Aug 1;22(15):5031-4. doi: 10.1016/j.bmcl.2012.06.012. Epub 2012 Jun 13.

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

Author information

1
Pharmaceutical Chemistry Division, Institute of Pharmacy, University of Hamburg, Hamburg, Germany. finn.hansen@hhu.de

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.

PMID:
22749420
DOI:
10.1016/j.bmcl.2012.06.012
[Indexed for MEDLINE]

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