Abstract
To identify new cost-effective prostaglandin D₂ (DP) receptor antagonists, a series of novel 3-benzoylaminophenylacetic acids were synthesized and biologically evaluated. Among those tested, some representative compounds were found to be orally available. Receptor selectivity and rat PK profiles were also evaluated. The structure-activity relationship (SAR) study is presented.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Benzamides / chemical synthesis
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Benzamides / chemistry
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Benzamides / pharmacology*
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Binding, Competitive / drug effects
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CHO Cells
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Cricetinae
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Dose-Response Relationship, Drug
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Drug Design*
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Male
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Molecular Conformation
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Phenylacetates / chemical synthesis
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Phenylacetates / chemistry
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Phenylacetates / pharmacology*
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Rats
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Receptors, Immunologic / antagonists & inhibitors*
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Receptors, Prostaglandin / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
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Tissue Distribution
Substances
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Benzamides
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Phenylacetates
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Receptors, Immunologic
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Receptors, Prostaglandin
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prostaglandin D2 receptor