… -substituted aminosulfonyl)-1, 2, 3, 4-tetrahydroisoquinoline Inhibitors of Phenylethanolamine N-Methyltransferase that Display Remarkable Potency and Selectivity 1

GL Grunewald, FA Romero…

Index: Grunewald, Gary L.; Romero, F. Anthony; Criscione, Kevin R. Journal of Medicinal Chemistry, 2005 , vol. 48, # 1 p. 134 - 140

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Citation Number: 20

Abstract

Six 3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1, 2, 3, 4-tetrahydroisoquinolines (16- 21) were synthesized and evaluated for their phenylethanolamine N-methyltransferase (PNMT) inhibitory potency and affinity for the α2-adrenoceptor. The addition of nonpolar substituents to the sulfonamide nitrogen of 9 (3-CH2OH-7-SO2NH2-THIQ) led to inhibitors (16-21) that have high PNMT inhibitory potency and high selectivity, and most of these (16 ...