Title of article
Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity
Author/Authors
Gavin A. Whitlock، نويسنده , , Paul V. Fish، نويسنده , , M. Jonathan Fray، نويسنده , , Alan Stobie، نويسنده , , Florian Wakenhut، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
2896
To page
2899
Abstract
A novel series of pyridyl-phenyl ethers are disclosed, which possess dual 5-HT and NA reuptake pharmacology with good selectivity over dopamine reuptake inhibition. An analysis of the relationship between lipophilicity and pharmacology highlighted that potent dual SNRI activity was only achievable at c log P > 3.5. The series was found to possess significant polypharmacology issues, and we concluded that this off-target promiscuity was related to lipophilicity.
Keywords
Pyridyl-phenyl ether , 5-HT reuptake , NA reuptake , Lipophilicity , Polypharmacology , Off-target promiscuity
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799468
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