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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

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

doi

10.1016/j.bmcl.2012.06.012

subject

Has Abstract

pub_date

2012-08-01 00:00:00

pages

5031-4

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00759-7

journal_volume

22

pub_type

杂志文章

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