Inhibitors of phenylethanolamine N-methyltransferase devoid of α 2-adrenoceptor affinity

GL Grunewald, J Lu, KR Criscione, CO Okoro

Index: Grunewald, Gary L.; Lu, Jian; Criscione, Kevin R.; Okoro, Cosmas O. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 23 p. 5319 - 5323

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Citation Number: 24

Abstract

A series of 3-trifluoromethyl-1, 2, 3, 4-tetrahydroisoquinolines was synthesized and evaluated for their phenylethanolamine N-methyltransferase (PNMT) inhibitory potency and affinity for the α2-adrenoceptor. Although their PNMT inhibitory potency decreased compared with corresponding 3-methyl-, 3-hydroxymethyl-or 3-unsubstituted-THIQs, some of them showed good selectivity due to their extremely low α2-adrenoceptor affinity.