Abstract
A series of inhibitors of mammalian 15-lipoxygenase (15-LO) based on a 3,4,5-tri-substituted pyrazole scaffold is described. Replacement of a sulfonamide functionality in the lead series with a sulfamide group resulted in improved physicochemical properties generating analogs with enhanced inhibition in cell-based and whole blood assays.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Amides / chemical synthesis
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Amides / chemistry*
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Amides / pharmacology
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Animals
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Arachidonate 15-Lipoxygenase / chemistry*
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Arachidonate 15-Lipoxygenase / metabolism
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CHO Cells
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Cricetinae
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Cricetulus
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Humans
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Hydroxyeicosatetraenoic Acids / blood
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Lipoxygenase Inhibitors / chemical synthesis
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Lipoxygenase Inhibitors / chemistry*
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Lipoxygenase Inhibitors / pharmacology
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Pyrazoles / chemistry*
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Rabbits
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry
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Sulfonamides / pharmacology
Substances
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Amides
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Hydroxyeicosatetraenoic Acids
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Lipoxygenase Inhibitors
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Pyrazoles
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Sulfonamides
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pyrazole
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15-hydroxy-5,8,11,13-eicosatetraenoic acid
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Arachidonate 15-Lipoxygenase