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
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
Journal title :
Bioorganic & Medicinal Chemistry Letters
