Abstract
The identification and structure-activity relationships of 2-aminomethyl-1-aryl cyclopropane carboxamides as novel NK(3) receptor antagonists are reported. The compound series was optimized to give analogues with low nanomolar binding to the NK(3) receptor and brain exposure, leading to activity in vivo in the senktide-induced hypoactivity model in gerbils.
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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Carboxylic Acids* / chemical synthesis
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Carboxylic Acids* / chemistry
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Carboxylic Acids* / pharmacology
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Cyclopropanes / chemical synthesis*
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Cyclopropanes / chemistry
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Cyclopropanes / pharmacology
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Disease Models, Animal
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Gerbillinae
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Molecular Structure
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Peptides / chemical synthesis
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Peptides / chemistry
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Peptides / pharmacology
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Receptors, Neurokinin-3 / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Amides
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Carboxylic Acids
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Cyclopropanes
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Peptides
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Receptors, Neurokinin-3