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.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Arachidonate 5-Lipoxygenase / chemistry*
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Arachidonate 5-Lipoxygenase / metabolism
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Carboxylic Acids / chemical synthesis
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Carboxylic Acids / chemistry
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Carboxylic Acids / metabolism
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Cyclooxygenase 1 / chemistry*
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Cyclooxygenase 1 / metabolism
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Cyclooxygenase Inhibitors / chemical synthesis*
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Cyclooxygenase Inhibitors / chemistry
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Cyclooxygenase Inhibitors / metabolism
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Lipoxygenase Inhibitors / chemical synthesis*
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Lipoxygenase Inhibitors / chemistry
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Lipoxygenase Inhibitors / metabolism
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Protein Binding
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Structure-Activity Relationship
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Thiophenes / chemical synthesis
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Thiophenes / chemistry*
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Thiophenes / metabolism
Substances
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6-chloro-3-hydroxybenzo(b)thiophene-2-carboxylic acid
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Carboxylic Acids
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Cyclooxygenase Inhibitors
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Lipoxygenase Inhibitors
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Thiophenes
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benzothiophene
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2-thiophene carboxylic acid
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Arachidonate 5-Lipoxygenase
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Cyclooxygenase 1