Abstract
Novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives were identified as potent human H(3) receptor inverse agonists. After systematic modification of lead 5a, the potent and selective analog 5r was identified. Elimination of hERG K(+) channel and human alpha(1A)-adrenoceptor activities is the main focus of the present study.
MeSH terms
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Administration, Oral
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Adrenergic alpha-1 Receptor Antagonists*
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Brain / drug effects
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Combinatorial Chemistry Techniques
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Dose-Response Relationship, Drug
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels / antagonists & inhibitors*
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Histamine Agonists / pharmacology*
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Humans
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Molecular Structure
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Quinazolinones / chemistry
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Quinazolinones / pharmacology*
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Structure-Activity Relationship
Substances
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Adrenergic alpha-1 Receptor Antagonists
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels
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Histamine Agonists
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KCNH2 protein, human
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Quinazolinones