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  • Title: Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.
    Author: Grunewald GL, Romero FA, Seim MR, Criscione KR, Deupree JD, Spackman CC, Bylund DB.
    Journal: Bioorg Med Chem Lett; 2005 Feb 15; 15(4):1143-7. PubMed ID: 15686930.
    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 alpha(2)-adrenoceptor. Although alpha(2)-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.
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