Title of article
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines
Author/Authors
Joanne M. Caine and Gary L. Grunewald، نويسنده , , F. Anthony Romero، نويسنده , , Mitchell R. Seim، نويسنده , , Kevin R. Criscione، نويسنده , , Jean D. Deupree، نويسنده , , Christy C. Spackman، نويسنده , , David B. Bylund، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
1143
To page
1147
Abstract
3-Hydroxyethyl- and 3-hydroxypropyl-7-substituted-tetrahydroisoquinolines (9, 10, 16, and 17) were synthesized and evaluated for their phenylethanolamine N-methyltransferase (PNMT) inhibitory potency and affinity for the α2-adrenoceptor. Although α2-adrenoceptor affinity decreased for these compounds, selectivity was not gained over the parent 3-hydroxymethyl compounds (1, 2) due to a loss in PNMT inhibitory potency.
Keywords
Phenylethanolamine N-methyltransferase , Enzyme inhibitors , tetrahydroisoquinoline , structure-based design
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795353
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