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Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Grunewald GL,Romero FA,Seim MR,Criscione KR,Deupree JD,Spackman CC,Bylund DB

doi

10.1016/j.bmcl.2004.12.013

subject

Has Abstract

pub_date

2005-02-15 00:00:00

pages

1143-7

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01472-6

journal_volume

15

pub_type

杂志文章

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